High Throughput Screening Facility

Sarah J Harmych , Thomas P Hasaka , Vivian Truong Jones , Joshua A Bauer , Bhuminder Singh.  Protocol for high-throughput drug screening in 384-well 3D collagen cultures of SC colorectal cancer cells using colony morphology as a readout. PMID: 41468265. DOI: 10.1016/j.xpro.2025.104300

Amporndanai K, Katinas JM, Chopra A, Kayode O, Vadukoot AK, Waterson AG, Fesik SW. NMR-Based Fragment Screen of the von Hippel-Lindau Elongin C&B Complex. ACS Med Chem Lett. 2025;16(8):1648-54. doi: 10.1021/acsmedchemlett.5c00316. PubMed PMID: 40832550; PMCID: PMC12358976.

Arora K, Sheehy TL, Schulman JA, Kimmel BR, McAtee C, Bharti V, Weaver AM, Wilson JT. Macromolecular Diamidobenzimidazole Conjugates Activate STING. bioRxiv. 2025. doi: 10.1101/2025.01.21.634206. PubMed PMID: 39896685; PMCID: PMC11785100.

Castiglione GM, Chen X, Xu Z, Dbouk NH, Bose AA, Carmona-Berrio D, Chi EE, Zhou L, Boronina TN, Cole RN, Wu S, Liu AD, Liu TD, Lu H, Kalbfleisch T, Rinker D, Rokas A, Ortved K, Duh EJ. Running a genetic stop sign accelerates oxygen metabolism and energy production in horses. Science. 2025;387(6741):eadr8589. doi: 10.1126/science.adr8589. PubMed PMID: 40146832.

Duncan RA, Haymer DH, Lazarenko RM, Li L, Blackwell Y, Days EL, Krishnan S, Gray AT, Boutaud O, Engers DW, Lindsley CW, Denton JS, Bender AM. Characterization of Next-Generation Inhibitors for the Inward-Rectifier Potassium Channel K(ir)2.1: Discovery of VU6080824. ACS Med Chem Lett. 2025;16(9):1762-71. doi: 10.1021/acsmedchemlett.5c00297. PubMed PMID: 40959251; PMCID: PMC12434521.

Harmych SJ, Hasaka TP, Sievers CK, Kang SW, Ramirez MA, Jones VT, Zhao Z, Kovtun O, Wahoski CC, Liu Q, Lau KS, Coffey RJ, Bauer JA, Singh B. 3D collagen high-throughput screen identifies drugs that induce epithelial polarity and enhance chemotherapy response in colorectal cancer. Commun Biol. 2025;8(1):1261. doi: 10.1038/s42003-025-08699-0. PubMed PMID: 40847193.

Jia G, Chen Z, Ping J, Cai Q, Tao R, Li C, Bauer JA, Xie Y, Ambs S, Barnard ME, Chen Y, Choi JY, Gao YT, Garcia-Closas M, Gu J, Hu JJ, Iwasaki M, John EM, Kweon SS, Li CI, Matsuda K, Matsuo K, Nathanson KL, Nemesure B, Olopade OI, Pal T, Park SK, Park B, Press MF, Sanderson M, Sandler DP, Shen CY, Troester MA, Yao S, Zheng Y, Ahearn T, Brewster AM, Falusi A, Hennis AJM, Ito H, Kubo M, Lee ES, Makumbi T, Ndom P, Noh DY, O'Brien KM, Ojengbede O, Olshan AF, Park MH, Reid S, Yamaji T, Zirpoli G, Butler EN, Huang M, Low SK, Obafunwa J, Weinberg CR, Zhang H, Zhao H, Cote ML, Ambrosone CB, Huo D, Li B, Kang D, Palmer JR, Shu XO, Haiman CA, Guo X, Long J, Zheng W. Refining breast cancer genetic risk and biology through multi-ancestry fine-mapping analyses of 192 risk regions. Nat Genet. 2025;57(1):80-7. doi: 10.1038/s41588-024-02031-y. PubMed PMID: 39753771; PMCID: PMC12184877.

Katinas JM, Amporndanai K, Taylor AJ, Rose KL, Gareiss PC, Crespo RA, Phan J, Waterson AG, Fesik SW. Nuclear Magnetic Resonance-based fragment screen of the E3 ligase Fem-1 homolog B. Protein Sci. 2025;34(12):e70365. doi: 10.1002/pro.70365. PubMed PMID: 41229306; PMCID: PMC12612594.

McBride MA, Caja KR, Patil TK, Owen AM, Luan L, Bohannon JK, Hernandez A, Stothers CL, Trenary IA, Rahim M, Young JD, Calcutt MW, Stephens VR, Davis X, Oliver MA, Hao D, Si C, McRae M, Nguyen KK, Davis NS, Wang J, Patil NK, Sherwood ER. Immunoresponsive gene 1 facilitates TLR4 agonist-induced augmentation of innate antimicrobial immunity. J Leukoc Biol. 2025;117(2). doi: 10.1093/jleuko/qiae198. PubMed PMID: 39351765; PMCID: PMC11879002.

Moster KRC, Vanoye CG, Chang-Gonzalez AC, Romaine IM, Stefanski KM, Wilkinson MC, Bauer JA, Hasaka TP, Days EL, Desai RR, Butcher KR, Sulikowski GA, Waterson AG, Meiler J, Ledwitch KV, George AL, Jr., Sanders CR. High Throughput Screening Identifies a Small Molecule Trafficking Corrector for Long-QT Syndrome Associated KCNQ1 Variants. bioRxiv. 2025. doi: 10.1101/2025.10.13.682066. PubMed PMID: 41279429; PMCID: PMC12632771.

Stefanski KM, Huang H, Luu DD, Hutchison JM, Saksena N, Fisch AJ, Hasaka TP, Bauer JA, Kenworthy AK, Van Horn WD, Sanders CR. Pharmacological Tools to Modulate Ordered Membrane Domains and Order-Dependent Protein Function. bioRxiv. 2025. doi: 10.1101/2025.10.03.680351. PubMed PMID: 41256712; PMCID: PMC12622036.

Tanaka M, Sekioka Y, Hashimoto G, Mori T, Shono T, Isaji Y, Hisaichi K, Childress ES, Bollinger S, Schmitt JA, Chopko TC, Garrison AT, Perry CK, Chronister K, Kramer M, Chang S, Watson KJ, Dickerson JW, Bubser M, Rook JM, Jones CK, Boutaud O, Bridges TM, Denton JS, Engers DW, Kurata H, Lindsley CW. Optimization of Selective and CNS Penetrant Alkyne-Based TREK Inhibitors: The Discovery and Characterization of ONO-9517601 (VU6022856) and ONO-7927846 (VU6024391). J Med Chem. 2025;68(21):23554-72. doi: 10.1021/acs.jmedchem.5c02535. PubMed PMID: 41104520; PMCID: PMC12621189.

Webb EM, Seymour K, Hamm HE. Trypsin Activates Human Platelets via Proteolytic Cleavage of Protease-Activated Receptor 4. Thromb Haemost. 2025. doi: 10.1055/a-2747-9083. PubMed PMID: 41248893.

Brookens SK, Cho SH, Paik Y, Meyer K, Raybuck AL, Park C, Greenwood DL, Rathmell JC, Boothby MR. Plasma Cell Differentiation, Antibody Quality, and Initial Germinal Center B Cell Population Depend on Glucose Influx Rate. J Immunol. 2024;212(1):43-56. doi: 10.4049/jimmunol.2200756. PubMed PMID: 37955416; PMCID: PMC10841396.

Bullock KK, Hasaka T, Days E, Bauer JA, Ward PA, Richmond A. A High-Throughput Immune-Oncology Screen Identifies Immunostimulatory Properties of Cytotoxic Chemotherapy Agents in TNBC. Cancers (Basel). 2024;16(23). doi: 10.3390/cancers16234075. PubMed PMID: 39682260; PMCID: PMC11639798.

Carvajal-Garcia J, Bracey H, Johnson AE, Hernandez Viera AJ, Egli M, Simsek EN, Jaremba EA, Kim K, Merrikh H. A small molecule that inhibits the evolution of antibiotic resistance. NAR Mol Med. 2024;1(1):ugae001. doi: 10.1093/narmme/ugae001. PubMed PMID: 38911259; PMCID: PMC11188740.

Cho SH, Jones MA, Meyer K, Anderson DM, Chetyrkin S, Calcutt MW, Caprioli RM, Semenkovich CF, Boothby MR. B cell expression of the enzyme PexRAP, an intermediary in ether lipid biosynthesis, promotes antibody responses and germinal center size. bioRxiv. 2024. doi: 10.1101/2024.10.17.618760. PubMed PMID: 39464149; PMCID: PMC11507954.

Li GC, Castro MA, Ukwaththage T, Sanders CR. Optimizing NMR fragment-based drug screening for membrane protein targets. J Struct Biol X. 2024;9:100100. doi: 10.1016/j.yjsbx.2024.100100. PubMed PMID: 38883400; PMCID: PMC11176934.

Li K, McClenahan SJ, Han C, Bungard JD, Rathnayake U, Boutaud O, Bauer JA, Days EL, Lindsley CW, Shelton EL, Denton JS. Discovery and Characterization of VU0542270, the First Selective Inhibitor of Vascular Kir6.1/SUR2B K(ATP) Channels. Mol Pharmacol. 2024;105(3):202-12. doi: 10.1124/molpharm.123.000783. PubMed PMID: 38302135; PMCID: PMC10877733.

Ma JG, O'Neill MJ, Richardson E, Thomson KL, Ingles J, Muhammad A, Solus JF, Davogustto G, Anderson KC, Shoemaker MB, Stergachis AB, Floyd BJ, Dunn K, Parikh VN, Chubb H, Perrin MJ, Roden DM, Vandenberg JI, Ng CA, Glazer AM. Multisite Validation of a Functional Assay to Adjudicate SCN5A Brugada Syndrome-Associated Variants. Circ Genom Precis Med. 2024;17(4):e004569. doi: 10.1161/CIRCGEN.124.004569. PubMed PMID: 38953211; PMCID: PMC11335442.

McBride MA, Stothers CL, Fensterheim BA, Caja KR, Owen AM, Hernandez A, Bohannon JK, Patil NK, Ali S, Dalal S, Rahim M, Trenary IA, Young JD, Williams DL, Sherwood ER. Bacteria- and fungus-derived PAMPs induce innate immune memory via similar functional, metabolic, and transcriptional adaptations. J Leukoc Biol. 2024;115(2):358-73. doi: 10.1093/jleuko/qiad120. PubMed PMID: 37793181; PMCID: PMC10872320.

Meyer CT, Smith BN, Wang J, Teuscher KB, Grieb BC, Howard GC, Silver AJ, Lorey SL, Stott GM, Moore WJ, Lee T, Savona MR, Weissmiller AM, Liu Q, Quaranta V, Fesik SW, Tansey WP. Expanded profiling of WD repeat domain 5 inhibitors reveals actionable strategies for the treatment of hematologic malignancies. Proc Natl Acad Sci U S A. 2024;121(35):e2408889121. doi: 10.1073/pnas.2408889121. PubMed PMID: 39167600; PMCID: PMC11363251.

O'Neill MJ, Ng CA, Aizawa T, Sala L, Bains S, Winbo A, Ullah R, Shen Q, Tan CY, Kozek K, Vanags LR, Mitchell DW, Shen A, Wada Y, Kashiwa A, Crotti L, Dagradi F, Musu G, Spazzolini C, Neves R, Bos JM, Giudicessi JR, Bledsoe X, Gamazon ER, Lancaster M, Glazer AM, Knollmann BC, Roden DM, Weile J, Roth F, Salem JE, Earle N, Stiles R, Agee T, Johnson CN, Horie M, Skinner J, Ackerman MJ, Schwartz PJ, Ohno S, Vandenberg JI, Kroncke BM. Multiplexed Assays of Variant Effect and Automated Patch-clamping Improve KCNH2-LQTS Variant Classification and Cardiac Event Risk Stratification. medRxiv. 2024. doi: 10.1101/2024.02.01.24301443. PubMed PMID: 38370760; PMCID: PMC10871451.

Qunies AM, Spitznagel BD, Du Y, Peprah PK, Mohamed YK, Weaver CD, Emmitte KA. Structure-Activity Relationship Studies in a Series of Xanthine Inhibitors of SLACK Potassium Channels. Molecules. 2024;29(11). doi: 10.3390/molecules29112437. PubMed PMID: 38893312; PMCID: PMC11173529.

Stauffer PE, Brinkley J, Jacobson DA, Quaranta V, Tyson DR. Purinergic Ca(2+) Signaling as a Novel Mechanism of Drug Tolerance in BRAF-Mutant Melanoma. Cancers (Basel). 2024;16(13). doi: 10.3390/cancers16132426. PubMed PMID: 39001489; PMCID: PMC11240618.

Subati T, Yang Z, Murphy MB, Stark JM, Trykall DZ, Davies SS, Barnett JV, Murray KT. Isolevuglandins Promote Mitochondrial Dysfunction and Electrophysiologic Abnormalities in Atrial Cardiomyocytes. Cells. 2024;13(6). doi: 10.3390/cells13060483. PubMed PMID: 38534327; PMCID: PMC10969716.

Tarr JC, Salovich JM, Aichinger M, Jeon K, Veerasamy N, Sensintaffar JL, Arnhof H, Samwer M, Christov PP, Kim K, Wunberg T, Schweifer N, Trapani F, Arnold A, Martin F, Zhao B, Miriyala N, Sgubin D, Fogarty S, Moore WJ, Stott GM, Olejniczak ET, Engelhardt H, Rudolph D, Lee T, McConnell DB, Fesik SW. Discovery of a Myeloid Cell Leukemia 1 (Mcl-1) Inhibitor That Demonstrates Potent In Vivo Activities in Mouse Models of Hematological and Solid Tumors. J Med Chem. 2024;67(16):14370-93. doi: 10.1021/acs.jmedchem.4c01188. PubMed PMID: 39102508; PMCID: PMC11345828 was funded by Boehringer Ingelheim. M. Aichinger, H. Arnhof, M. Samwer, T. Wunberg, F. Trapani, F. Martin, H. Engelhardt, and D. Rudolph are employees of Boehringer Ingelheim. N. Schweifer and D. McConnell are former employees of Boehringer Ingelheim.

Tateishi Y, Webb SN, Li B, Liu L, Lindsey Rose K, Leser M, Patel P, Guengerich FP. Proteomics, modeling, and fluorescence assays delineate cytochrome b(5) residues involved in binding and stimulation of cytochrome P450 17A1 17,20-lyase. J Biol Chem. 2024;300(3):105688. doi: 10.1016/j.jbc.2024.105688. PubMed PMID: 38280431; PMCID: PMC10878793.

Taylor AJ, Amporndanai K, Rietz TA, Zhao B, Thiruvaipati A, Wei Q, South TM, Crow MM, Apakama C, Sensintaffar JL, Phan J, Lee T, Fesik SW. Fragment-Based Screen of SARS-CoV-2 Papain-like Protease (PL(pro)). ACS Med Chem Lett. 2024;15(8):1351-7. doi: 10.1021/acsmedchemlett.4c00238. PubMed PMID: 39140055; PMCID: PMC11318101.

Williams D, Hargrove-Wiley E, Bindeman W, Valent D, Miranda AX, Beckstead J, Fingleton B. Type II Interleukin-4 Receptor Activation in Basal Breast Cancer Cells Promotes Tumor Progression via Metabolic and Epigenetic Modulation. Int J Mol Sci. 2024;25(9). doi: 10.3390/ijms25094647. PubMed PMID: 38731867; PMCID: PMC11083536.

Bender AM, Valentine MS, Bauer JA, Days E, Lindsley CW, Merryman WD. Identification of Potent, Selective, and Peripherally Restricted Serotonin Receptor 2B Antagonists from a High-Throughput Screen. Assay Drug Dev Technol. 2023;21(3):89-96. doi: 10.1089/adt.2022.116. PubMed PMID: 36930852; PMCID: PMC10122230.

Carroll DT, Elsakr JM, Miller A, Fuhr J, Lindsley SR, Kirigiti M, Takahashi DL, Dean TA, Wesolowski SR, McCurdy CE, Friedman JE, Aagaard KM, Kievit P, Gannon M. Maternal Western-style diet in nonhuman primates leads to offspring islet adaptations including altered gene expression and insulin hypersecretion. Am J Physiol Endocrinol Metab. 2023;324(6):E577-E88. doi: 10.1152/ajpendo.00087.2023. PubMed PMID: 37134140; PMCID: PMC10259856.

Dodd CJ, Chronister KS, Rathnayake U, Parr LC, Li K, Chang S, Mi D, Days EL, Bauer JA, Cho HP, Boutaud O, Denton JS, Lindsley CW, Han C. Synthesis and SAR of a novel Kir6.2/SUR1 channel opener scaffold identified by HTS. Bioorg Med Chem Lett. 2023;87:129256. doi: 10.1016/j.bmcl.2023.129256. PubMed PMID: 36966977; PMCID: PMC10395071.

Liu D, Ceddia RP, Zhang W, Shi F, Fang H, Collins S. Discovery of another mechanism for the inhibition of particulate guanylyl cyclases by the natriuretic peptide clearance receptor. Proc Natl Acad Sci U S A. 2023;120(28):e2307882120. doi: 10.1073/pnas.2307882120. PubMed PMID: 37399424; PMCID: PMC10334801.

Malabanan MM, Chapagain P, Haratipour Z, Choi WJ, Orun AR, Blind RD. New High-Throughput Screen Discovers Novel Ligands of Full-Length Nuclear Receptor LRH-1. ACS Chem Biol. 2023;18(5):1101-14. doi: 10.1021/acschembio.2c00805. PubMed PMID: 37074920; PMCID: PMC10404069.

Qunies AM, Spitznagel BD, Du Y, David Weaver C, Emmitte KA. Design, synthesis, and biological evaluation of a novel series of 1,2,4-oxadiazole inhibitors of SLACK potassium channels: Identification of in vitro tool VU0935685. Bioorg Med Chem. 2023;95:117487. doi: 10.1016/j.bmc.2023.117487. PubMed PMID: 37812884; PMCID: PMC10842602.

Schuss C, Vu O, Mishra NM, Tough IR, Du Y, Stichel J, Cox HM, Weaver CD, Meiler J, Emmitte KA, Beck-Sickinger AG. Structure-Activity Relationship Study of the High-Affinity Neuropeptide Y(4) Receptor Positive Allosteric Modulator VU0506013. J Med Chem. 2023;66(13):8745-66. doi: 10.1021/acs.jmedchem.3c00383. PubMed PMID: 37339079.

Shi F, de Fatima Silva F, Liu D, Patel HU, Xu J, Zhang W, Turk C, Kruger M, Collins S. Salt-inducible kinase inhibition promotes the adipocyte thermogenic program and adipose tissue browning. Mol Metab. 2023;74:101753. doi: 10.1016/j.molmet.2023.101753. PubMed PMID: 37321371; PMCID: PMC10319839.

Shi Y, Katdare KA, Kim H, Rosch JC, Neal EH, Vafaie-Partin S, Bauer JA, Lippmann ES. An arrayed CRISPR knockout screen identifies genetic regulators of GLUT1 expression. Sci Rep. 2023;13(1):21038. doi: 10.1038/s41598-023-48361-5. PubMed PMID: 38030680; PMCID: PMC10687026.

Siricilla S, Hansen CJ, Rogers JH, De D, Simpson CL, Waterson AG, Sulikowski GA, Crockett SL, Boatwright N, Reese J, Paria BC, Newton J, Herington JL. Arrest of mouse preterm labor until term delivery by combination therapy with atosiban and mundulone, a natural product with tocolytic efficacy. Pharmacol Res. 2023;195:106876. doi: 10.1016/j.phrs.2023.106876. PubMed PMID: 37536638; PMCID: PMC10712649.

Talati M, Brittain E, Agrawal V, Fortune N, Simon K, Shay S, Zeng X, Freeman ML, West J, Hemnes A. A potential adverse role for leptin and cardiac leptin receptor in the right ventricle in pulmonary arterial hypertension: effect of metformin is BMPR2 mutation-specific. Front Med (Lausanne). 2023;10:1276422. doi: 10.3389/fmed.2023.1276422. PubMed PMID: 37869164; PMCID: PMC10586504.

Teuscher KB, Mills JJ, Tian J, Han C, Meyers KM, Sai J, South TM, Crow MM, Van Meveren M, Sensintaffar JL, Zhao B, Amporndanai K, Moore WJ, Stott GM, Tansey WP, Lee T, Fesik SW. Structure-Based Discovery of Potent, Orally Bioavailable Benzoxazepinone-Based WD Repeat Domain 5 Inhibitors. J Med Chem. 2023;66(24):16783-806. doi: 10.1021/acs.jmedchem.3c01529. PubMed PMID: 38085679.

Zarrow JE, Alli-Oluwafuyi AM, Youwakim CM, Kim K, Jenkins AN, Suero IC, Jones MR, Mashhadi Z, Mackie K, Waterson AG, Doran AC, Sulikowski GA, Davies SS. Small Molecule Activation of NAPE-PLD Enhances Efferocytosis by Macrophages. ACS Chem Biol. 2023;18(8):1891-904. doi: 10.1021/acschembio.3c00401. PubMed PMID: 37531659; PMCID: PMC10443532 A.W.G., A.M.D., G.A.S., and S.S.D. are named as inventors on a patent application for the use of benzothiazole phenylsulfonyl-piperidine carboxamides as small molecule NAPE-PLD activators. This work was funded in part by grants from the NIH/NHLBI P01HL116263 (S.S.D. and A.C.D.) and by an American Heart Association fellowship 835504 (J.E.Z.).

Bergdorf K, Bauer JA, Westover D, Phifer C, Murphy B, Tyson DR, Lee E, Weiss VL. Utilizing Three-Dimensional Culture Methods to Improve High-Throughput Drug Screening in Anaplastic Thyroid Carcinoma. Cancers (Basel). 2022;14(8). doi: 10.3390/cancers14081855. PubMed PMID: 35454763; PMCID: PMC9031362.

Cukier HN, Kim H, Griswold AJ, Codreanu SG, Prince LM, Sherrod SD, McLean JA, Dykxhoorn DM, Ess KC, Hedera P, Bowman AB, Neely MD. Genomic, transcriptomic, and metabolomic profiles of hiPSC-derived dopamine neurons from clinically discordant brothers with identical PRKN deletions. NPJ Parkinsons Dis. 2022;8(1):84. doi: 10.1038/s41531-022-00346-3. PubMed PMID: 35768426; PMCID: PMC9243035.

Cumberbatch D, Mori T, Yang J, Mi D, Vinson P, Weaver CD, Johnson CH. A BRET Ca(2+) sensor enables high-throughput screening in the presence of background fluorescence. Sci Signal. 2022;15(747):eabq7618. doi: 10.1126/scisignal.abq7618. PubMed PMID: 35973028; PMCID: PMC9930640.

Egly CL, Blackwell DJ, Schmeckpeper J, Delisle BP, Weaver CD, Knollmann BC. A High-Throughput Screening Assay to Identify Drugs that Can Treat Long QT Syndrome Caused by Trafficking-Deficient K(V)11.1 (hERG) Variants. Mol Pharmacol. 2022;101(4):236-45. doi: 10.1124/molpharm.121.000421. PubMed PMID: 35125346; PMCID: PMC9638947.

Figueroa EE, Denton JS. A SWELL time to develop the molecular pharmacology of the volume-regulated anion channel (VRAC). Channels (Austin). 2022;16(1):27-36. doi: 10.1080/19336950.2022.2033511. PubMed PMID: 35114895; PMCID: PMC8820792.

Fricke N, Raghunathan K, Tiwari A, Stefanski KM, Balakrishnan M, Waterson AG, Capone R, Huang H, Sanders CR, Bauer JA, Kenworthy AK. High-Content Imaging Platform to Discover Chemical Modulators of Plasma Membrane Rafts. ACS Cent Sci. 2022;8(3):370-8. doi: 10.1021/acscentsci.1c01058. PubMed PMID: 35355811; PMCID: PMC8961798.

Garrison AT, Orsi DL, Capstick RA, Whomble D, Li J, Carter TR, Felts AS, Vinson PN, Rodriguez AL, Han A, Hajari K, Cho HP, Teal LB, Ragland MG, Ghamari-Langroudi M, Bubser M, Chang S, Schnetz-Boutaud NC, Boutaud O, Blobaum AL, Foster DJ, Niswender CM, Conn PJ, Lindsley CW, Jones CK, Han C. Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M(5) Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder. J Med Chem. 2022;65(8):6273-86. doi: 10.1021/acs.jmedchem.2c00192. PubMed PMID: 35417155.

Glazer AM, Davogustto G, Shaffer CM, Vanoye CG, Desai RR, Farber-Eger EH, Dikilitas O, Shang N, Pacheco JA, Yang T, Muhammad A, Mosley JD, Van Driest SL, Wells QS, Shaffer LL, Kalash OR, Wada Y, Bland HT, Yoneda ZT, Mitchell DW, Kroncke BM, Kullo IJ, Jarvik GP, Gordon AS, Larson EB, Manolio TA, Mirshahi T, Luo JZ, Schaid D, Namjou B, Alsaied T, Singh R, Singhal A, Liu C, Weng C, Hripcsak G, Ralston JD, McNally EM, Chung WK, Carrell DS, Leppig KA, Hakonarson H, Sleiman P, Sohn S, Glessner J, e MN, Denny J, Wei WQ, George AL, Jr., Shoemaker MB, Roden DM. Arrhythmia Variant Associations and Reclassifications in the eMERGE-III Sequencing Study. Circulation. 2022;145(12):877-91. doi: 10.1161/CIRCULATIONAHA.121.055562. PubMed PMID: 34930020; PMCID: PMC8940719.

Gulsevin A, Glazer AM, Shields T, Kroncke BM, Roden DM, Meiler J. Veratridine Can Bind to a Site at the Mouth of the Channel Pore at Human Cardiac Sodium Channel Na(V)1.5. Int J Mol Sci. 2022;23(4). doi: 10.3390/ijms23042225. PubMed PMID: 35216338; PMCID: PMC8878851.

Hanna A, Nixon MJ, Estrada MV, Sanchez V, Sheng Q, Opalenik SR, Toren AL, Bauer J, Owens P, Mason FM, Cook RS, Sanders ME, Arteaga CL, Balko JM. Combined Dusp4 and p53 loss with Dbf4 amplification drives tumorigenesis via cell cycle restriction and replication stress escape in breast cancer. Breast Cancer Res. 2022;24(1):51. doi: 10.1186/s13058-022-01542-y. PubMed PMID: 35850776; PMCID: PMC9290202.

Huang S, Shu X, Ping J, Wu J, Wang J, Shidal C, Guo X, Bauer JA, Long J, Shu XO, Zheng W, Cai Q. TBX1 functions as a putative oncogene of breast cancer through promoting cell cycle progression. Carcinogenesis. 2022;43(1):12-20. doi: 10.1093/carcin/bgab111. PubMed PMID: 34919666; PMCID: PMC8832409.

Kelly KP, Borsetti H, Wenzler ME, Ustione A, Kim K, Christov PP, Ramirez B, Bauer JA, Piston DW, Johnson CH, Sulikowski GA. Screen for Small-Molecule Modulators of Circadian Rhythms Reveals Phenazine as a Redox-State Modifying Clockwork Tuner. ACS Chem Biol. 2022;17(7):1658-64. doi: 10.1021/acschembio.2c00240. PubMed PMID: 35679588; PMCID: PMC9398883.

Lyu W, Mi D, Vinson PN, Xiao Y, Zhang G. Large-Scale Identification of Multiple Classes of Host Defense Peptide-Inducing Compounds for Antimicrobial Therapy. Int J Mol Sci. 2022;23(15). doi: 10.3390/ijms23158400. PubMed PMID: 35955551; PMCID: PMC9368921.

McClenahan SJ, Kent CN, Kharade SV, Isaeva E, Williams JC, Han C, Terker A, Gresham R, 3rd, Lazarenko RM, Days EL, Romaine IM, Bauer JA, Boutaud O, Sulikowski GA, Harris R, Weaver CD, Staruschenko A, Lindsley CW, Denton JS. VU6036720: The First Potent and Selective In Vitro Inhibitor of Heteromeric Kir4.1/5.1 Inward Rectifier Potassium Channels. Mol Pharmacol. 2022;101(5):357-70. doi: 10.1124/molpharm.121.000464. PubMed PMID: 35246480; PMCID: PMC9092466.

O'Neill MJ, Muhammad A, Li B, Wada Y, Hall L, Solus JF, Short L, Roden DM, Glazer AM. Dominant negative effects of SCN5A missense variants. Genet Med. 2022;24(6):1238-48. doi: 10.1016/j.gim.2022.02.010. PubMed PMID: 35305865; PMCID: PMC9262418.

Prael FJ, Kim K, Du Y, Spitznagel BD, Sulikowski GA, Delpire E, Weaver CD. Discovery of Small Molecule KCC2 Potentiators Which Attenuate In Vitro Seizure-Like Activity in Cultured Neurons. Front Cell Dev Biol. 2022;10. doi: ARTN 912812.10.3389/fcell.2022.912812. PubMed PMID: WOS:000826983100001.

Qunies AM, Mishra NM, Spitznagel BD, Du Y, Acuna VS, David Weaver C, Emmitte KA. Structure-activity relationship studies in a new series of 2-amino-N-phenylacetamide inhibitors of Slack potassium channels. Bioorg Med Chem Lett. 2022;76:129013. doi: 10.1016/j.bmcl.2022.129013. PubMed PMID: 36184030; PMCID: PMC10230575.

Thoner TW, Jr., Meloy MM, Long JM, Diller JR, Slaughter JC, Ogden KM. Reovirus Efficiently Reassorts Genome Segments during Coinfection and Superinfection. J Virol. 2022;96(18):e0091022. doi: 10.1128/jvi.00910-22. PubMed PMID: 36094315; PMCID: PMC9517712.

Wandishin CM, Robbins CJ, Tyson DR, Harris LA, Quaranta V. Real-time luminescence enables continuous drug-response analysis in adherent and suspension cell lines. Cancer Biol Ther. 2022;23(1):358-68. doi: 10.1080/15384047.2022.2065182. PubMed PMID: 35443861; PMCID: PMC9037430.

Zhang Z, Zhang W, Blakes R, Sundby LJ, Shi Z, Rockey DC, Ervasti JM, Nam YJ. Fibroblast fate determination during cardiac reprogramming by remodeling of actin filaments. Stem Cell Reports. 2022;17(7):1604-19. doi: 10.1016/j.stemcr.2022.05.004. PubMed PMID: 35688153; PMCID: PMC9287671.

Bertron JL, Duvernay MT, Mitchell SG, Smith ST, Maeng JG, Blobaum AL, Davis DC, Meiler J, Hamm HE, Lindsley CW. Discovery and Optimization of a Novel Series of Competitive and Central Nervous System-Penetrant Protease-Activated Receptor 4 (PAR4) Inhibitors. ACS Chem Neurosci. 2021;12(24):4524-34. doi: 10.1021/acschemneuro.1c00557. PubMed PMID: 34855359; PMCID: PMC8823334.

Diana Neely M, Xie S, Prince LM, Kim H, Tukker AM, Aschner M, Thimmapuram J, Bowman AB. Single cell RNA sequencing detects persistent cell type- and methylmercury exposure paradigm-specific effects in a human cortical neurodevelopmental model. Food Chem Toxicol. 2021;154:112288. doi: 10.1016/j.fct.2021.112288. PubMed PMID: 34089799.

Engdahl TB, Kuzmina NA, Ronk AJ, Mire CE, Hyde MA, Kose N, Josleyn MD, Sutton RE, Mehta A, Wolters RM, Lloyd NM, Valdivieso FR, Ksiazek TG, Hooper JW, Bukreyev A, Crowe JE, Jr. Broad and potently neutralizing monoclonal antibodies isolated from human survivors of New World hantavirus infection. Cell Rep. 2021;35(5):109086. doi: 10.1016/j.celrep.2021.109086. PubMed PMID: 33951434; PMCID: PMC8142553.

Figueroa EE, Denton JS. Zinc pyrithione activates the volume-regulated anion channel through an antioxidant-sensitive mechanism. Am J Physiol Cell Physiol. 2021;320(6):C1088-C98. doi: 10.1152/ajpcell.00070.2021. PubMed PMID: 33826406; PMCID: PMC8285639.

Kozek K, Wada Y, Sala L, Denjoy I, Egly C, O'Neill MJ, Aiba T, Shimizu W, Makita N, Ishikawa T, Crotti L, Spazzolini C, Kotta MC, Dagradi F, Castelletti S, Pedrazzini M, Gnecchi M, Leenhardt A, Salem JE, Ohno S, Zuo Y, Glazer AM, Mosley JD, Roden DM, Knollmann BC, Blume JD, Extramiana F, Schwartz PJ, Horie M, Kroncke BM. Estimating the Post-Test Probability of Long QT Syndrome Diagnosis for Rare KCNH2 Variants. Circ Genom Precis Med. 2021. doi: 10.1161/CIRCGEN.120.003289. PubMed PMID: 34309407.

Lubbock ALR, Harris LA, Quaranta V, Tyson DR, Lopez CF. Thunor: visualization and analysis of high-throughput dose-response datasets. Nucleic Acids Res. 2021;49(W1):W633-W40. doi: 10.1093/nar/gkab424. PubMed PMID: 34038546; PMCID: PMC8265171.

Prince LM, Neely MD, Warren EB, Thomas MG, Henley MR, Smith KK, Aschner M, Bowman AB. Environmentally relevant developmental methylmercury exposures alter neuronal differentiation in a human-induced pluripotent stem cell model. Food Chem Toxicol. 2021;152:112178. doi: 10.1016/j.fct.2021.112178. PubMed PMID: 33831500.

Redman-Rivera LN, Shaver TM, Jin H, Marshall CB, Schafer JM, Sheng Q, Hongo RA, Beckermann KE, Wheeler FC, Lehmann BD, Pietenpol JA. Acquisition of aneuploidy drives mutant p53-associated gain-of-function phenotypes. Nat Commun. 2021;12(1):5184. doi: 10.1038/s41467-021-25359-z. PubMed PMID: 34465782; PMCID: PMC8408227.

Salem JE, Yang T, Moslehi JJ, Waintraub X, Gandjbakhch E, Bachelot A, Hidden-Lucet F, Hulot JS, Knollmann BC, Lebrun-Vignes B, Funck-Brentano C, Glazer AM, Roden DM. Androgenic effects on ventricular repolarization: A translational study from the international pharmacovigilance database to iPSC-cardiomyocytes. Ann Endocrinol (Paris). 2021;82(3-4):132-3. doi: 10.1016/j.ando.2020.02.008. PubMed PMID: 32171470.

Schuss C, Vu O, Schubert M, Du Y, Mishra NM, Tough IR, Stichel J, Weaver CD, Emmitte KA, Cox HM, Meiler J, Beck-Sickinger AG. Highly Selective Y4 Receptor Antagonist Binds in an Allosteric Binding Pocket. J Med Chem. 2021;64(5):2801-14. doi: 10.1021/acs.jmedchem.0c02000. PubMed PMID: 33595306.

Sharma S, Lesiak L, Aretz CD, Du Y, Kumar S, Gautam N, Alnouti Y, Dhuria NV, Chhonker YS, Weaver CD, Hopkins CR. Discovery, synthesis and biological characterization of a series of N-(1-(1,1-dioxidotetrahydrothiophen-3-yl)-3-methyl-1H-pyrazol-5-yl)acetamide ethers as novel GIRK1/2 potassium channel activators. RSC Med Chem. 2021;12(8):1366-73. doi: 10.1039/d1md00129a. PubMed PMID: 34458739; PMCID: PMC8372201 the Panoptic kinetic imaging plate reader and the thallium-sensitive fluorescent indicators used in these studies.

Shidal C, Shu X, Wu J, Wang J, Huang S, Long J, Bauer JA, Ping J, Guo X, Zheng W, Shu XO, Cai Q. Functional Genomic Analyses of the 21q22.3 Locus Identifying Functional Variants and Candidate Gene YBEY for Breast Cancer Risk. Cancers (Basel). 2021;13(9). doi: 10.3390/cancers13092037. PubMed PMID: 33922500; PMCID: PMC8122893.

Smith SC, Gribble J, Diller JR, Wiebe MA, Thoner TW, Jr., Denison MR, Ogden KM. Reovirus RNA recombination is sequence directed and generates internally deleted defective genome segments during passage. J Virol. 2021. doi: 10.1128/JVI.02181-20. PubMed PMID: 33472930; PMCID: PMC8103698.

Zhang Z, Villalpando J, Zhang W, Nam YJ. Chamber-Specific Protein Expression during Direct Cardiac Reprogramming. Cells. 2021;10(6). doi: 10.3390/cells10061513. PubMed PMID: 34208439; PMCID: PMC8234528.

Agarwal R, Bensing BA, Mi D, Vinson PN, Baudry J, Iverson TM, Smith JC. Structure based virtual screening identifies small molecule effectors for the sialoglycan binding protein Hsa. Biochem J. 2020;477(19):3695-707. doi: 10.1042/BCJ20200332. PubMed PMID: 32910185.

Aggarwal G, Zarrow JE, Mashhadi Z, Flynn CR, Vinson P, Weaver CD, Davies SS. Symmetrically substituted dichlorophenes inhibit N-acyl-phosphatidylethanolamine phospholipase D. J Biol Chem. 2020;295(21):7289-300. doi: 10.1074/jbc.RA120.013362. PubMed PMID: 32284327; PMCID: PMC7247316.

Bergdorf K, Phifer C, Bharti V, Westover D, Bauer J, Vilgelm A, Lee E, Weiss V. High-throughput drug screening of fine-needle aspiration-derived cancer organoids. STAR Protoc. 2020;1(3):100212. doi: 10.1016/j.xpro.2020.100212. PubMed PMID: 33377106; PMCID: PMC7757655.

Diller JR, Halloran SR, Koehler M, Dos Santos Natividade R, Alsteens D, Stehle T, Dermody TS, Ogden KM. Reovirus sigma1 Conformational Flexibility Modulates the Efficiency of Host Cell Attachment. J Virol. 2020;94(23). doi: 10.1128/JVI.01163-20. PubMed PMID: 32938765; PMCID: PMC7654274.

Glazer AM, Kroncke BM, Matreyek KA, Yang T, Wada Y, Shields T, Salem JE, Fowler DM, Roden DM. Deep Mutational Scan of an SCN5A Voltage Sensor. Circ Genom Precis Med. 2020;13(1):e002786. doi: 10.1161/CIRCGEN.119.002786. PubMed PMID: 31928070; PMCID: PMC7031040.

Glazer AM, Wada Y, Li B, Muhammad A, Kalash OR, O'Neill MJ, Shields T, Hall L, Short L, Blair MA, Kroncke BM, Capra JA, Roden DM. High-Throughput Reclassification of SCN5A Variants. Am J Hum Genet. 2020;107(1):111-23. doi: 10.1016/j.ajhg.2020.05.015. PubMed PMID: 32533946; PMCID: PMC7332654.

Horning KJ, Joshi P, Nitin R, Balachandran RC, Yanko FM, Kim K, Christov P, Aschner M, Sulikowski GA, Weaver CD, Bowman AB. Identification of a selective manganese ionophore that enables nonlethal quantification of cellular manganese. J Biol Chem. 2020;295(12):3875-90. doi: 10.1074/jbc.RA119.009781. PubMed PMID: 32047113; PMCID: PMC7086026.

Jia D, Paudel BB, Hayford CE, Hardeman KN, Levine H, Onuchic JN, Quaranta V. Drug-Tolerant Idling Melanoma Cells Exhibit Theory-Predicted Metabolic Low-Low Phenotype. Front Oncol. 2020;10:1426. doi: 10.3389/fonc.2020.01426. PubMed PMID: 32923395; PMCID: PMC7457027.

Juttukonda LJ, Beavers WN, Unsihuay D, Kim K, Pishchany G, Horning KJ, Weiss A, Al-Tameemi H, Boyd JM, Sulikowski GA, Bowman AB, Skaar EP. A Small-Molecule Modulator of Metal Homeostasis in Gram-Positive Pathogens. mBio. 2020;11(5). doi: 10.1128/mBio.02555-20. PubMed PMID: 33109764; PMCID: PMC7593973.

Kozek KA, Glazer AM, Ng CA, Blackwell D, Egly CL, Vanags LR, Blair M, Mitchell D, Matreyek KA, Fowler DM, Knollmann BC, Vandenberg JI, Roden DM, Kroncke BM. High-throughput discovery of trafficking-deficient variants in the cardiac potassium channel KV11.1. Heart Rhythm. 2020;17(12):2180-9. doi: 10.1016/j.hrthm.2020.05.041. PubMed PMID: 32522694; PMCID: PMC7704534.

Kroncke BM, Smith DK, Zuo Y, Glazer AM, Roden DM, Blume JD. A Bayesian method to estimate variant-induced disease penetrance. PLoS Genet. 2020;16(6):e1008862. doi: 10.1371/journal.pgen.1008862. PubMed PMID: 32569262; PMCID: PMC7347235.

Lee MA, Bergdorf KN, Phifer CJ, Jones CY, Byon SY, Sawyer LM, Bauer JA, Weiss VL. Novel three-dimensional cultures provide insights into thyroid cancer behavior. Endocr Relat Cancer. 2020;27(2):111-21. doi: 10.1530/ERC-19-0374. PubMed PMID: 31804972; PMCID: PMC7295136.

Rundo L, Tangherloni A, Tyson DR, Betta R, Militello C, Spolaor S, Nobile MS, Besozzi D, Lubbock ALR, Quaranta V, Mauri G, Lopez CF, Cazzaniga P. ACDC: Automated Cell Detection and Counting for Time-Lapse Fluorescence Microscopy. Appl Sci (Basel). 2020;10(18). doi: 10.3390/app10186187. PubMed PMID: 34306736; PMCID: PMC8297459.

Schafer JM, Lehmann BD, Gonzalez-Ericsson PI, Marshall CB, Beeler JS, Redman LN, Jin H, Sanchez V, Stubbs MC, Scherle P, Johnson KN, Sheng Q, Roland JT, Bauer JA, Shyr Y, Chakravarthy B, Mobley BC, Hiebert SW, Balko JM, Sanders ME, Liu PCC, Pietenpol JA. Targeting MYCN-expressing triple-negative breast cancer with BET and MEK inhibitors. Sci Transl Med. 2020;12(534). doi: 10.1126/scitranslmed.aaw8275. PubMed PMID: 32161105; PMCID: PMC7427123.

Spitznagel BD, Mishra NM, Qunies AM, Prael FJ, 3rd, Du Y, Kozek KA, Lazarenko RM, Denton JS, Emmitte KA, Weaver CD. VU0606170, a Selective Slack Channels Inhibitor, Decreases Calcium Oscillations in Cultured Cortical Neurons. ACS Chem Neurosci. 2020;11(21):3658-71. doi: 10.1021/acschemneuro.0c00583. PubMed PMID: 33143429.

Streeten EA, See VY, Jeng LBJ, Maloney KA, Lynch M, Glazer AM, Yang T, Roden D, Pollin TI, Daue M, Ryan KA, Van Hout C, Gosalia N, Gonzaga-Jauregui C, Economides A, Perry JA, O'Connell J, Beitelshees A, Palmer K, Mitchell BD, Shuldiner AR, Regeneron Genetics C. KCNQ1 and Long QT Syndrome in 1/45 Amish: The Road From Identification to Implementation of Culturally Appropriate Precision Medicine. Circ Genom Precis Med. 2020;13(6):e003133. doi: 10.1161/CIRCGEN.120.003133. PubMed PMID: 33141630; PMCID: PMC7748050.

Vilgelm AE, Bergdorf K, Wolf M, Bharti V, Shattuck-Brandt R, Blevins A, Jones C, Phifer C, Lee M, Lowe C, Hongo R, Boyd K, Netterville J, Rohde S, Idrees K, Bauer JA, Westover D, Reinfeld B, Baregamian N, Richmond A, Rathmell WK, Lee E, McDonald OG, Weiss VL. Fine-Needle Aspiration-Based Patient-Derived Cancer Organoids. iScience. 2020;23(8):101408. doi: 10.1016/j.isci.2020.101408. PubMed PMID: 32771978; PMCID: PMC7415927.

Wages PA, Joshi P, Tallman KA, Kim HH, Bowman AB, Porter NA. Screening ToxCast for Chemicals That Affect Cholesterol Biosynthesis: Studies in Cell Culture and Human Induced Pluripotent Stem Cell-Derived Neuroprogenitors. Environ Health Perspect. 2020;128(1):17014. doi: 10.1289/EHP5053. PubMed PMID: 31985273; PMCID: PMC7015578.

Zhang Z, Nam YJ. Assessing Cardiac Reprogramming using High Content Imaging Analysis. J Vis Exp. 2020(164). doi: 10.3791/61859. PubMed PMID: 33165328; PMCID: PMC7988430.

Abney KK, Bubser M, Du Y, Kozek KA, Bridges TM, Linsdley CW, Daniels JS, Morrison RD, Wickman K, Hopkins CR, Jones CK, Weaver CD. Analgesic Effects of the GIRK Activator, VU0466551, Alone and in Combination with Morphine in Acute and Persistent Pain Models. ACS Chem Neurosci. 2019;10(3):1294-9. doi: 10.1021/acschemneuro.8b00370. PubMed PMID: 30474955; PMCID: PMC6765219.

Afzal A, Figueroa EE, Kharade SV, Bittman K, Matlock BK, Flaherty DK, Denton JS. The LRRC8 volume-regulated anion channel inhibitor, DCPIB, inhibits mitochondrial respiration independently of the channel. Physiol Rep. 2019;7(23):e14303. doi: 10.14814/phy2.14303. PubMed PMID: 31814333; PMCID: PMC6900491.

Aho ER, Wang J, Gogliotti RD, Howard GC, Phan J, Acharya P, Macdonald JD, Cheng K, Lorey SL, Lu B, Wenzel S, Foshage AM, Alvarado J, Wang F, Shaw JG, Zhao B, Weissmiller AM, Thomas LR, Vakoc CR, Hall MD, Hiebert SW, Liu Q, Stauffer SR, Fesik SW, Tansey WP. Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity. Cell Rep. 2019;26(11):2916-28 e13. doi: 10.1016/j.celrep.2019.02.047. PubMed PMID: 30865883; PMCID: PMC6448596.

Aretz C, Morwitzer MJ, Sanford A, Hogan AM, Portillo M, Kharade SV, Kramer M, McArthey J, Trigueros RR, Piermarini PM, Denton JS, Hopkins CR. Discovery and characterization of 2-nitro-5-(4-(phenylsulfonyl)piperazin-1-yl)-N-(pyridin-4-ylmethyl)anilines as novel inhibitors of the Aedes aegypti Kir1 (AeKir1) channel. ACS Infect Dis. 2019. doi: 10.1021/acsinfecdis.8b00368. PubMed PMID: 30832472.

Chavali NV, Kryshtal DO, Parikh SS, Wang L, Glazer AM, Blackwell DJ, Kroncke BM, Shoemaker MB, Knollmann BC. Patient-independent human induced pluripotent stem cell model: A new tool for rapid determination of genetic variant pathogenicity in long QT syndrome. Heart Rhythm. 2019;16(11):1686-95. doi: 10.1016/j.hrthm.2019.04.031. PubMed PMID: 31004778; PMCID: PMC6935564.

Chen R, Prael F, Li Z, Delpire E, Weaver CD, Swale D. Functional Coupling of K+-Cl- Cotransporter (KCC) to GABA-Gated Cl- Channels in the Central Nervous System of Drosophila melanogaster leads to altered drug sensitivities. ACS Chem Neurosci. 2019. doi: 10.1021/acschemneuro.8b00697. PubMed PMID: 30942574.

Diller JR, Parrington HM, Patton JT, Ogden KM. Rotavirus Species B Encodes a Functional Fusion-Associated Small Transmembrane Protein. J Virol. 2019;93(20). doi: 10.1128/JVI.00813-19. PubMed PMID: 31375572; PMCID: PMC6798121.

Dumas ME, Chen GY, Kendrick ND, Xu G, Larsen SD, Jana S, Waterson AG, Bauer JA, Hancock W, Sulikowski GA, Ohi R. Dual inhibition of Kif15 by oxindole and quinazolinedione chemical probes. Bioorg Med Chem Lett. 2019;29(2):148-54. doi: 10.1016/j.bmcl.2018.12.008. PubMed PMID: 30528696; PMCID: PMC6681659.

Figueroa EE, Kramer M, Strange K, Denton JS. CysLT1 receptor antagonists pranlukast and zafirlukast inhibit LRRC8-mediated volume regulated anion channels independently of the receptor. Am J Physiol Cell Physiol. 2019;317(4):C857-C66. doi: 10.1152/ajpcell.00281.2019. PubMed PMID: 31390227; PMCID: PMC6850990.

Formisano L, Lu Y, Servetto A, Hanker AB, Jansen VM, Bauer JA, Sudhan DR, Guerrero-Zotano AL, Croessmann S, Guo Y, Ericsson PG, Lee KM, Nixon MJ, Schwarz LJ, Sanders ME, Dugger TC, Cruz MR, Behdad A, Cristofanilli M, Bardia A, O'Shaughnessy J, Nagy RJ, Lanman RB, Solovieff N, He W, Miller M, Su F, Shyr Y, Mayer IA, Balko JM, Arteaga CL. Aberrant FGFR signaling mediates resistance to CDK4/6 inhibitors in ER+ breast cancer. Nat Commun. 2019;10(1):1373. doi: 10.1038/s41467-019-09068-2. PubMed PMID: 30914635; PMCID: PMC6435685.

Fulton MG, Loch MT, Cuoco CA, Rodriguez AL, Days E, Vinson PN, Kozek KA, Weaver CD, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Challenges in the Discovery and Optimization of mGlu2/4 Heterodimer Positive Allosteric Modulators. Lett Drug Des Discov. 2019;16(12):1387-94. doi: 10.2174/1570180815666181017131349. PubMed PMID: 32201485; PMCID: PMC7059629.

Guo Y, Sui JY, Kim K, Zhang Z, Qu XA, Nam YJ, Willette RN, Barnett JV, Knollmann BC, Force T, Lal H. Cardiomyocyte Homeodomain-Interacting Protein Kinase 2 Maintains Basal Cardiac Function via Extracellular Signal-Regulated Kinase Signaling. Circulation. 2019;140(22):1820-33. doi: 10.1161/CIRCULATIONAHA.119.040740. PubMed PMID: 31581792; PMCID: PMC7219521.

Kharade SV, Sanchez-Andres JV, Fulton MG, Shelton EJ, Blobaum AL, Engers DW, Hofmann CS, Dadi PK, Lantier L, Jacobson DA, Lindsley CW, Denton JS. Structure-activity relationships, pharmacokinetics, and pharmacodynamics of the Kir6.2/SUR1-specific channel opener, VU0071063. J Pharmacol Exp Ther. 2019. doi: 10.1124/jpet.119.257204. PubMed PMID: 31201216.

Kozek KA, Du Y, Sharma S, Prael FJ, 3rd, Spitznagel BD, Kharade SV, Denton JS, Hopkins CR, Weaver CD. Discovery and Characterization of VU0529331, a Synthetic Small-Molecule Activator of Homomeric G Protein-Gated, Inwardly Rectifying, Potassium (GIRK) Channels. ACS Chem Neurosci. 2019;10(1):358-70. doi: 10.1021/acschemneuro.8b00287. PubMed PMID: 30136838; PMCID: PMC6528656.

Lee T, Christov PP, Shaw S, Tarr JC, Zhao B, Veerasamy N, Jeon KO, Mills JJ, Bian Z, Sensintaffar JL, Arnold AL, Fogarty SA, Perry E, Ramsey HE, Cook R, Hollingshead M, Davis Millin M, Lee KM, Koss B, Budhraja A, Opferman JT, Kim K, Arteaga CL, Moore WJ, Olejniczak ET, Savona MR, Fesik SW. Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors that Demonstrate in vivo Activity in Mouse Xenograft Models of Human Cancer. J Med Chem. 2019. doi: 10.1021/acs.jmedchem.8b01991. PubMed PMID: 30929420.

Lehman JM, Hoeksema MD, Staub J, Qian J, Harris B, Callison JC, Miao J, Shi C, Eisenberg R, Chen H, Chen SC, Massion PP. Somatostatin receptor 2 signaling promotes growth and tumor survival in small-cell lung cancer. Int J Cancer. 2019;144(5):1104-14. doi: 10.1002/ijc.31771. PubMed PMID: 30152518; PMCID: PMC6448409.

Macdonald JD, Chacon Simon S, Han C, Wang F, Shaw JG, Howes JE, Sai J, Yuh JP, Camper D, Alicie BM, Alvarado J, Nikhar S, Payne W, Aho ER, Bauer JA, Zhao B, Phan J, Thomas LR, Rossanese OW, Tansey WP, Waterson AG, Stauffer SR, Fesik SW. Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction. J Med Chem. 2019;62(24):11232-59. doi: 10.1021/acs.jmedchem.9b01411. PubMed PMID: 31724864; PMCID: PMC6933084.

McClure R, Redha R, Vinson P, Pham W. A Robust and Scalable High-Throughput Compatible Assay for Screening Amyloid-beta-Binding Compounds. J Alzheimers Dis. 2019;70(1):187-97. doi: 10.3233/JAD-190316. PubMed PMID: 31177230; PMCID: PMC6943818.

Meyer CT, Wooten DJ, Paudel BB, Bauer J, Hardeman KN, Westover D, Lovly CM, Harris LA, Tyson DR, Quaranta V. Quantifying Drug Combination Synergy along Potency and Efficacy Axes. Cell Syst. 2019;8(2):97-108 e16. doi: 10.1016/j.cels.2019.01.003. PubMed PMID: 30797775; PMCID: PMC6675406.

Mistry AM, Wooten DJ, Davis LT, Mobley BC, Quaranta V, Ihrie RA. Ventricular-Subventricular Zone Contact by Glioblastoma is Not Associated with Molecular Signatures in Bulk Tumor Data. Sci Rep. 2019;9(1):1842. doi: 10.1038/s41598-018-37734-w. PubMed PMID: 30755636; PMCID: PMC6372607.

Porter JD, Vivas O, Weaver CD, Alsafran A, DiMilo E, Arnold LA, Dickson EJ, Dockendorff C. An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders. Bioorg Med Chem Lett. 2019;29(23):126681. doi: 10.1016/j.bmcl.2019.126681. PubMed PMID: 31668424; PMCID: PMC6858848.

Sharma S, Kozek KA, Abney KK, Kumar S, Gautam N, Alnouti Y, David Weaver C, Hopkins CR. Discovery, synthesis and characterization of a series of (1-alkyl-3-methyl-1H-pyrazol-5-yl)-2-(5-aryl-2H-tetrazol-2-yl)acetamides as novel GIRK1/2 potassium channel activators. Bioorg Med Chem Lett. 2019;29(6):791-6. doi: 10.1016/j.bmcl.2019.01.027. PubMed PMID: 30718161; PMCID: PMC6398930.

Siricilla S, Knapp KM, Rogers JH, Berger C, Shelton EL, Mi D, Vinson P, Condon J, Paria BC, Reese J, Sheng Q, Herington JL. Comparative analysis of myometrial and vascular smooth muscle cells to determine optimal cells for use in drug discovery. Pharmacol Res. 2019:104268. doi: 10.1016/j.phrs.2019.104268. PubMed PMID: 31078743.

Trads JB, Hull K, Matsuura BS, Laprell L, Fehrentz T, Gorldt N, Kozek KA, Weaver CD, Klocker N, Barber DM, Trauner D. Sign Inversion in Photopharmacology: Incorporation of Cyclic Azobenzenes in Photoswitchable Potassium Channel Blockers and Openers. Angew Chem Int Ed Engl. 2019;58(43):15421-8. doi: 10.1002/anie.201905790. PubMed PMID: 31441199.

Vo BN, Abney KK, Anderson A, Marron Fernandez de Velasco E, Benneyworth MA, Daniels JS, Morrison RD, Hopkins CR, Weaver CD, Wickman K. VU0810464, a non-urea GIRK channel activator, exhibits enhanced selectivity for neuronal GIRK channels and reduces stress-induced hyperthermia in mice. Br J Pharmacol. 2019. doi: 10.1111/bph.14671. PubMed PMID: 30924523.

Wooten DJ, Groves SM, Tyson DR, Liu Q, Lim JS, Albert R, Lopez CF, Sage J, Quaranta V. Systems-level network modeling of Small Cell Lung Cancer subtypes identifies master regulators and destabilizers. PLoS Comput Biol. 2019;15(10):e1007343. doi: 10.1371/journal.pcbi.1007343. PubMed PMID: 31671086; PMCID: PMC6860456 following competing interests: J.S. receives research funding from StemCentrx/Abbvie, Revolution Medicines, and from Pfizer, and owns stock in Forty Seven Inc.

Wu L, Wang J, Cai Q, Cavazos TB, Emami NC, Long J, Shu XO, Lu Y, Guo X, Bauer JA, Pasaniuc B, Penney KL, Freedman ML, Kote-Jarai Z, Witte JS, Haiman CA, Eeles RA, Zheng W, and the Practical CBPCCPC. Identification of Novel Susceptibility Loci and Genes for Prostate Cancer Risk: A Transcriptome-Wide Association Study in Over 140,000 European Descendants. Cancer Res. 2019;79(13):3192-204. doi: 10.1158/0008-5472.CAN-18-3536. PubMed PMID: 31101764; PMCID: PMC6606384.

Abbott JR, Hodges TR, Daniels RN, Patel PA, Kennedy JP, Howes JE, Akan DT, Burns MC, Sai J, Sobolik T, Beesetty Y, Lee T, Rossanese OW, Phan J, Waterson AG, Fesik SW. Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling. J Med Chem. 2018. doi: 10.1021/acs.jmedchem.8b00360. PubMed PMID: 29856609.

Abney KK, Ramos-Hunter SJ, Romaine IM, Goodwin JS, Sulikowski GA, Weaver CD. Selective Activation of N,N'-Diacyl Rhodamine Pro-fluorophores Paired with Releasing Enzyme, Porcine Liver Esterase (PLE). Chemistry. 2018;24(36):8985-8. doi: 10.1002/chem.201801409. PubMed PMID: 29679472; PMCID: PMC6035858.

Burns MC, Howes JE, Sun Q, Little AJ, Camper DV, Abbott JR, Phan J, Lee T, Waterson AG, Rossanese OW, Fesik SW. High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and perturb RAS signaling. Anal Biochem. 2018;548:44-52. doi: 10.1016/j.ab.2018.01.025. PubMed PMID: 29444450; PMCID: PMC5935105.

Dietrich MH, Ogden KM, Long JM, Ebenhoch R, Thor A, Dermody TS, Stehle T. Structural and Functional Features of the Reovirus sigma1 Tail. J Virol. 2018;92(14). doi: 10.1128/JVI.00336-18. PubMed PMID: 29695426; PMCID: PMC6026731.

Dutter BF, Ender A, Sulikowski GA, Weaver CD. Rhodol-based thallium sensors for cellular imaging of potassium channel activity. Org Biomol Chem. 2018;16(31):5575-9. doi: 10.1039/c8ob01098f. PubMed PMID: 30051127.

Fensterheim BA, Young JD, Luan L, Kleinbard RR, Stothers CL, Patil NK, McAtee-Pereira AG, Guo Y, Trenary I, Hernandez A, Fults JB, Williams DL, Sherwood ER, Bohannon JK. The TLR4 Agonist Monophosphoryl Lipid A Drives Broad Resistance to Infection via Dynamic Reprogramming of Macrophage Metabolism. J Immunol. 2018;200(11):3777-89. doi: 10.4049/jimmunol.1800085. PubMed PMID: 29686054; PMCID: PMC5964009.

Genaro-Mattos TC, Tallman KA, Allen LB, Anderson A, Mirnics K, Korade Z, Porter NA. Dichlorophenyl piperazines, including a recently-approved atypical antipsychotic, are potent inhibitors of DHCR7, the last enzyme in cholesterol biosynthesis. Toxicol Appl Pharmacol. 2018;349:21-8. doi: 10.1016/j.taap.2018.04.029. PubMed PMID: 29698737.

Grouthier V, Lebrun-Vignes B, Glazer AM, Touraine P, Funck-Brentano C, Pariente A, Courtillot C, Bachelot A, Roden DM, Moslehi JJ, Salem JE. Increased long QT and torsade de pointes reporting on tamoxifen compared with aromatase inhibitors. Heart. 2018;104(22):1859-63. doi: 10.1136/heartjnl-2017-312934. PubMed PMID: 29720397; PMCID: PMC8022857.

Johnson CN, Potet F, Thompson MK, Kroncke BM, Glazer AM, Voehler MW, Knollmann BC, George AL, Jr., Chazin WJ. A Mechanism of Calmodulin Modulation of the Human Cardiac Sodium Channel. Structure. 2018;26(5):683-94 e3. doi: 10.1016/j.str.2018.03.005. PubMed PMID: 29606593; PMCID: PMC5932218.

Kharade SV, Kurata H, Bender AM, Blobaum AL, Figueroa EE, Duran A, Kramer M, Days E, Vinson P, Flores D, Satlin LM, Meiler J, Weaver CD, Lindsley CW, Hopkins CR, Denton JS. Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992. Mol Pharmacol. 2018;94(2):926-37. doi: 10.1124/mol.118.112359. PubMed PMID: 29895592.

Knowlton JJ, Fernandez de Castro I, Ashbrook AW, Gestaut DR, Zamora PF, Bauer JA, Forrest JC, Frydman J, Risco C, Dermody TS. The TRiC chaperonin controls reovirus replication through outer-capsid folding. Nat Microbiol. 2018;3(4):481-93. doi: 10.1038/s41564-018-0122-x. PubMed PMID: 29531365; PMCID: PMC5874176.

Kozek KA, Du Y, Sharma S, Prael FJ, Spitznagel BD, Kharade SV, Denton JS, Hopkins CR, Weaver CD. Discovery and Characterization of VU0529331, a Synthetic Small-Molecule Activator of Homomeric G Protein-gated, Inwardly-rectifying, Potassium (GIRK) Channels. ACS Chem Neurosci. 2018. doi: 10.1021/acschemneuro.8b00287. PubMed PMID: 30136838.

Kroncke BM, Glazer AM, Smith DK, Blume JD, Roden DM. SCN5A (NaV1.5) Variant Functional Perturbation and Clinical Presentation: Variants of a Certain Significance. Circ Genom Precis Med. 2018;11(5):e002095. doi: 10.1161/CIRCGEN.118.002095. PubMed PMID: 29728395; PMCID: PMC5941942.

Prael FJ, Chen R, Li Z, Reed CW, Lindsley CW, Weaver CD, Swale DR. Use of chemical probes to explore the toxicological potential of the K+/Cl− cotransporter (KCC) as a novel insecticide target to control the primary vector of dengue and Zika virus, Aedes aegypti. Pesticide Biochemistry and Physiology. 2018. doi: https://doi.org/10.1016/j.pestbp.2018.03.019.

Raybuck AL, Cho SH, Li J, Rogers MC, Lee K, Williams CL, Shlomchik M, Thomas JW, Chen J, Williams JV, Boothby MR. B Cell-Intrinsic mTORC1 Promotes Germinal Center-Defining Transcription Factor Gene Expression, Somatic Hypermutation, and Memory B Cell Generation in Humoral Immunity. J Immunol. 2018;200(8):2627-39. doi: 10.4049/jimmunol.1701321. PubMed PMID: 29531165; PMCID: PMC5893413.

Roden DM, Glazer AM, Kroncke B. Arrhythmia genetics: Not dark and lite, but 50 shades of gray. Heart Rhythm. 2018;15(8):1231-2. doi: 10.1016/j.hrthm.2018.04.031. PubMed PMID: 29709575; PMCID: PMC6590670.

Rook JM, Bertron JL, Cho HP, Garcia-Barrantes PM, Moran SP, Maksymetz JT, Nance KD, Dickerson JW, Remke DH, Chang S, Harp JM, Blobaum AL, Niswender CM, Jones CK, Stauffer SR, Conn PJ, Lindsley CW. A Novel M1 PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity. ACS Chem Neurosci. 2018. doi: 10.1021/acschemneuro.8b00131. PubMed PMID: 29701957.

Salem JE, Waintraub X, Courtillot C, Shaffer CM, Gandjbakhch E, Maupain C, Moslehi JJ, Badilini F, Haroche J, Gougis P, Fressart V, Glazer AM, Hidden-Lucet F, Touraine P, Lebrun-Vignes B, Roden DM, Bachelot A, Funck-Brentano C. Hypogonadism as a Reversible Cause of Torsades de Pointes in Men. Circulation. 2018;138(1):110-3. doi: 10.1161/CIRCULATIONAHA.118.034282. PubMed PMID: 29967236; PMCID: PMC6053686.

Sammons MF, Kharade SV, Filipski KJ, Boehm M, Smith AC, Shavnya A, Fernando DP, Dowling MS, Carpino PA, Castle NA, Zellmer SG, Antonio BM, Gosset JR, Carlo A, Denton JS. Discovery and in Vitro Optimization of 3-Sulfamoylbenzamides as ROMK Inhibitors. ACS Med Chem Lett. 2018;9(2):125-30. doi: 10.1021/acsmedchemlett.7b00481. PubMed PMID: 29456800; PMCID: PMC5807870.

Shaw S, Bian Z, Zhao B, Tarr JC, Veerasamy N, Jeon KO, Belmar J, Arnold AL, Fogarty SA, Perry E, Sensintaffar JL, Camper DV, Rossanese OW, Lee T, Olejniczak ET, Fesik SW. Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors Using Structure-Based Design. J Med Chem. 2018;61(6):2410-21. doi: 10.1021/acs.jmedchem.7b01155. PubMed PMID: 29323899.

Sutherland DM, Aravamudhan P, Dietrich MH, Stehle T, Dermody TS. Reovirus Neurotropism and Virulence Are Dictated by Sequences in the Head Domain of the Viral Attachment Protein. J Virol. 2018;92(23). doi: 10.1128/JVI.00974-18. PubMed PMID: 30209169; PMCID: PMC6232475.

Wages PA, Kim HH, Korade Z, Porter NA. Identification and characterization of prescription drugs that change levels of 7-dehydrocholesterol and desmosterol. J Lipid Res. 2018;59(10):1916-26. doi: 10.1194/jlr.M086991. PubMed PMID: 30087204; PMCID: PMC6168312.

Wang F, Jeon KO, Salovich JM, Macdonald JD, Alvarado J, Gogliotti RD, Phan J, Olejniczak ET, Sun Q, Wang S, Camper D, Yuh JP, Shaw JG, Sai J, Rossanese OW, Tansey WP, Stauffer SR, Fesik SW. Discovery of Potent 2-Aryl-6,7-dihydro-5 H-pyrrolo[1,2- a]imidazoles as WDR5-WIN-Site Inhibitors Using Fragment-Based Methods and Structure-Based Design. J Med Chem. 2018;61(13):5623-42. doi: 10.1021/acs.jmedchem.8b00375. PubMed PMID: 29889518.

Zhang S, Zhao Y, Heaster TM, Fischer MA, Stengel KR, Zhou X, Ramsey H, Zhou MM, Savona MR, Skala MC, Hiebert SW. BET inhibitors reduce cell size and induce reversible cell cycle arrest in AML. J Cell Biochem. 2018. doi: 10.1002/jcb.28005. PubMed PMID: 30417424.

Abe M, Seto M, Gogliotti RG, Loch MT, Bollinger KA, Chang S, Engelberg EM, Luscombe VB, Harp JM, Bubser M, Engers DW, Jones CK, Rodriguez AL, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines. ACS Med Chem Lett. 2017;8(10):1110-5. doi: 10.1021/acsmedchemlett.7b00317. PubMed PMID: 29057060; PMCID: PMC5641958.

Azumaya CM, Days EL, Vinson PN, Stauffer S, Sulikowski G, Weaver CD, Nakagawa T. Screening for AMPA receptor auxiliary subunit specific modulators. PLoS One. 2017;12(3):e0174742. doi: 10.1371/journal.pone.0174742. PubMed PMID: 28358902.

Bewley BR, Spearing PK, Weiner RL, Luscombe VB, Zhan X, Chang S, Cho HP, Rodriguez AL, Niswender CM, Conn PJ, Bridges TM, Engers DW, Lindsley CW. Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core. Bioorg Med Chem Lett. 2017;27(18):4274-9. doi: 10.1016/j.bmcl.2017.08.043. PubMed PMID: 28866269; PMCID: PMC5688877.

Chen X, Austin ED, Talati M, Fessel JP, Farber-Eger EH, Brittain EL, Hemnes AR, Loyd JE, West J. Oestrogen inhibition reverses pulmonary arterial hypertension and associated metabolic defects. Eur Respir J. 2017;50(2). doi: 10.1183/13993003.02337-2016. PubMed PMID: 28775043.

Dadi PK, Vierra NC, Days E, Dickerson MT, Vinson PN, Weaver CD, Jacobson DA. Selective Small Molecule Activators of TREK-2 Channels Stimulate Dorsal Root Ganglion c-Fiber Nociceptor Two-Pore-Domain Potassium Channel Currents and Limit Calcium Influx. ACS Chem Neurosci. 2017;8(3):558-68. doi: 10.1021/acschemneuro.6b00301. PubMed PMID: 27805811.

Dietrich MH, Harprecht C, Stehle T. The bulky and the sweet: How neutralizing antibodies and glycan receptors compete for virus binding. Protein Sci. 2017;26(12):2342-54. doi: 10.1002/pro.3319. PubMed PMID: 28986957; PMCID: PMC5699497.

Dietrich MH, Ogden KM, Katen SP, Reiss K, Sutherland DM, Carnahan RH, Goff M, Cooper T, Dermody TS, Stehle T. Structural Insights into Reovirus σ1 Interactions with Two Neutralizing Antibodies. Journal of virology. 2017;91(4):e01621-16. doi: 10.1128/JVI.01621-16. PubMed PMID: 27928010.

Egnatchik RA, Brittain EL, Shah AT, Fares WH, Ford HJ, Monahan K, Kang CJ, Kocurek EG, Zhu S, Luong T, Nguyen TT, Hysinger E, Austin ED, Skala MC, Young JD, Roberts LJ, 2nd, Hemnes AR, West J, Fessel JP. Dysfunctional BMPR2 signaling drives an abnormal endothelial requirement for glutamine in pulmonary arterial hypertension. Pulm Circ. 2017;7(1):186-99. doi: 10.1086/690236. PubMed PMID: 28680578; PMCID: 5448547.

Fensterheim BA, Guo Y, Sherwood ER, Bohannon JK. The Cytokine Response to Lipopolysaccharide Does Not Predict the Host Response to Infection. J Immunol. 2017;198(8):3264-73. doi: 10.4049/jimmunol.1602106. PubMed PMID: 28275139; PMCID: 5380530.

Hanker AB, Brewer MR, Sheehan JH, Koch JP, Sliwoski GR, Nagy R, Lanman R, Berger MF, Hyman DM, Solit DB, He J, Miller V, Cutler RE, Jr., Lalani AS, Cross D, Lovly CM, Meiler J, Arteaga CL. An Acquired HER2(T798I) Gatekeeper Mutation Induces Resistance to Neratinib in a Patient with HER2 Mutant-Driven Breast Cancer. Cancer Discov. 2017;7(6):575-85. doi: 10.1158/2159-8290.CD-16-1431. PubMed PMID: 28274957; PMCID: PMC5457707.

Hanker AB, Garrett JT, Estrada MV, Moore PD, Ericsson PG, Koch JP, Langley E, Singh S, Kim PS, Frampton GM, Sanford E, Owens P, Becker J, Groseclose MR, Castellino S, Joensuu H, Huober J, Brase JC, Majjaj S, Brohee S, Venet D, Brown D, Baselga J, Piccart M, Sotiriou C, Arteaga CL. HER2-Overexpressing Breast Cancers Amplify FGFR Signaling upon Acquisition of Resistance to Dual Therapeutic Blockade of HER2. Clin Cancer Res. 2017;23(15):4323-34. doi: 10.1158/1078-0432.CCR-16-2287. PubMed PMID: 28381415; PMCID: PMC5540793.

Hardeman KN, Peng C, Paudel BB, Meyer CT, Luong T, Tyson DR, Young JD, Quaranta V, Fessel JP. Dependence On Glycolysis Sensitizes BRAF-mutated Melanomas For Increased Response To Targeted BRAF Inhibition. Sci Rep. 2017;7:42604. doi: 10.1038/srep42604. PubMed PMID: 28205616; PMCID: 5311997.

Ichihara E, Westover D, Meador CB, Yan Y, Bauer JA, Lu P, Ye F, Kulick A, de Stanchina E, McEwen R, Ladanyi M, Cross D, Pao W, Lovly CM. SFK/FAK Signaling Attenuates Osimertinib Efficacy in Both Drug-Sensitive and Drug-Resistant Models of EGFR-Mutant Lung Cancer. Cancer Res. 2017;77(11):2990-3000. doi: 10.1158/0008-5472.CAN-16-2300. PubMed PMID: 28416483; PMCID: 5467531.

Jansen VM, Bhola NE, Bauer JA, Formisano L, Lee KM, Hutchinson KE, Witkiewicz AK, Moore PD, Estrada MV, Sanchez V, Ericsson PG, Sanders ME, Pohlmann PR, Pishvaian MJ, Riddle DA, Dugger TC, Wei W, Knudsen ES, Arteaga CL. Kinome-Wide RNA Interference Screen Reveals a Role for PDK1 in Acquired Resistance to CDK4/6 Inhibition in ER-Positive Breast Cancer. Cancer Res. 2017;77(9):2488-99. doi: 10.1158/0008-5472.CAN-16-2653. PubMed PMID: 28249908; PMCID: 5421398.

Karnes JH, Bastarache L, Shaffer CM, Gaudieri S, Xu Y, Glazer AM, Mosley JD, Zhao S, Raychaudhuri S, Mallal S, Ye Z, Mayer JG, Brilliant MH, Hebbring SJ, Roden DM, Phillips EJ, Denny JC. Phenome-wide scanning identifies multiple diseases and disease severity phenotypes associated with HLA variants. Sci Transl Med. 2017;9(389). doi: 10.1126/scitranslmed.aai8708. PubMed PMID: 28490672; PMCID: PMC5563969.

Karnes JH, Shaffer CM, Bastarache L, Gaudieri S, Glazer AM, Steiner HE, Mosley JD, Mallal S, Denny JC, Phillips EJ, Roden DM. Comparison of HLA allelic imputation programs. PLoS One. 2017;12(2):e0172444. doi: 10.1371/journal.pone.0172444. PubMed PMID: 28207879; PMCID: PMC5312875.

Lee KM, Giltnane JM, Balko JM, Schwarz LJ, Guerrero-Zotano AL, Hutchinson KE, Nixon MJ, Estrada MV, Sanchez V, Sanders ME, Lee T, Gomez H, Lluch A, Perez-Fidalgo JA, Wolf MM, Andrejeva G, Rathmell JC, Fesik SW, Arteaga CL. MYC and MCL1 Cooperatively Promote Chemotherapy-Resistant Breast Cancer Stem Cells via Regulation of Mitochondrial Oxidative Phosphorylation. Cell Metab. 2017;26(4):633-47 e7. doi: 10.1016/j.cmet.2017.09.009. PubMed PMID: 28978427; PMCID: PMC5650077.

Nance KD, Days EL, Weaver CD, Coldren A, Farmer TD, Cho HP, Niswender CM, Blobaum AL, Niswender KD, Lindsley CW. Discovery of a novel series of orally bioavailable and CNS penetrant Glucagon-Like Peptide 1 Receptor (GLP-1R) non-competitive antagonists based on a 1,3-disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrim idine-2,4(1H,3H)-dione core. J Med Chem. 2017. doi: 10.1021/acs.jmedchem.6b01706. PubMed PMID: 28103022.

Neely MD, Davison CA, Aschner M, Bowman AB. From the Cover: Manganese and Rotenone-Induced Oxidative Stress Signatures Differ in iPSC-Derived Human Dopamine Neurons. Toxicol Sci. 2017;159(2):366-79. doi: 10.1093/toxsci/kfx145. PubMed PMID: 28962525; PMCID: PMC5837701.

Reed CW, McGowan KM, Spearing PK, Stansley BJ, Roenfanz HF, Engers DW, Rodriguez AL, Engelberg EM, Luscombe VB, Loch MT, Remke DH, Rook JM, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides. ACS Med Chem Lett. 2017;8(12):1326-30. doi: 10.1021/acsmedchemlett.7b00429. PubMed PMID: 29259756; PMCID: PMC5733308.

Schubert M, Stichel J, Du Y, Tough IR, Sliwoski G, Meiler J, Cox HM, Weaver CD, Beck-Sickinger AG. Identification and Characterization of the First Selective Y4 Receptor Positive Allosteric Modulator. J Med Chem. 2017;60(17):7605-12. doi: 10.1021/acs.jmedchem.7b00976. PubMed PMID: 28795803.

Warren EB, Aicher AE, Fessel JP, Konradi C. Mitochondrial DNA depletion by ethidium bromide decreases neuronal mitochondrial creatine kinase: Implications for striatal energy metabolism. PLoS One. 2017;12(12):e0190456. doi: 10.1371/journal.pone.0190456. PubMed PMID: 29287112; PMCID: PMC5747477.

Wells QS, Veatch OJ, Fessel JP, Joon AY, Levinson RT, Mosley JD, Held EP, Lindsay CS, Shaffer CM, Weeke PE, Glazer AM, Bersell KR, Van Driest SL, Karnes JH, Blair MA, Lagrone LW, Su YR, Bowton EA, Feng Z, Ky B, Lenihan DJ, Fisch MJ, Denny JC, Roden DM. Genome-wide association and pathway analysis of left ventricular function after anthracycline exposure in adults. Pharmacogenet Genomics. 2017;27(7):247-54. doi: 10.1097/FPC.0000000000000284. PubMed PMID: 28542097; PMCID: PMC5502740.

Wieting JM, Vadukoot AK, Sharma S, Abney KK, Bridges TM, Daniels JS, Morrison RD, Wickman K, Weaver CD, Hopkins CR. Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators. ACS Chem Neurosci. 2017;8(9):1873-9. doi: 10.1021/acschemneuro.7b00217. PubMed PMID: 28697302.

Zurawski Z, Page B, Chicka MC, Brindley RL, Wells CA, Preininger AM, Hyde K, Gilbert JA, Cruz-Rodriguez O, Currie KPM, Chapman ER, Alford S, Hamm HE. Gβγ directly modulates vesicle fusion by competing with synaptotagmin for binding to neuronal SNARE proteins embedded in membranes. Journal of Biological Chemistry. 2017. doi: 10.1074/jbc.M116.773523.

Barber DM, Schonberger M, Burgstaller J, Levitz J, Weaver CD, Isacoff EY, Baier H, Trauner D. Optical control of neuronal activity using a light-operated GIRK channel opener (LOGO). Chem Sci. 2016;7(3):2347-52. doi: 10.1039/C5SC04084A. PubMed PMID: 28090283; PMCID: PMC5234268.

Borza CM, Su Y, Tran TL, Yu L, Steyns N, Temple KJ, Skwark MJ, Meiler J, Lindsley CW, Hicks BR, Leitinger B, Zent R, Pozzi A. Discoidin domain receptor 1 kinase activity is required for regulating collagen IV synthesis. Matrix Biol. 2016. doi: 10.1016/j.matbio.2016.11.009. PubMed PMID: 27915093.

Cho SH, Raybuck AL, Stengel K, Wei M, Beck TC, Volanakis E, Thomas JW, Hiebert S, Haase VH, Boothby MR. Germinal centre hypoxia and regulation of antibody qualities by a hypoxia response system. Nature. 2016;537(7619):234-8. doi: 10.1038/nature19334. PubMed PMID: 27501247; PMCID: PMC5161594.

Harris LA, Frick PL, Garbett SP, Hardeman KN, Paudel BB, Lopez CF, Quaranta V, Tyson DR. An unbiased metric of antiproliferative drug effect in vitro. Nat Methods. 2016. doi: 10.1038/nmeth.3852. PubMed PMID: 27135974.

Kim HH, Korade Z, Tallman KA, Liu W, Weaver CD, Mirnics K, Porter NA. Inhibitors of 7-Dehydrocholesterol Reductase: Screening of a Collection of Pharmacologically Active Compounds in Neuro2a Cells. Chem Res Toxicol. 2016. doi: 10.1021/acs.chemrestox.6b00054. PubMed PMID: 27097157.

Korade Z, Kim H-YH, Tallman KA, Liu W, Koczok K, Balogh I, Xu L, Mirnics K, Porter NA. The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-deficient Neuro2a Cells and Human Fibroblasts. Journal of Medicinal Chemistry. 2016. doi: 10.1021/acs.jmedchem.5b01696.

Patrone JD, Pelz NF, Bates BS, Souza-Fagundes EM, Vangamudi B, Camper DV, Kuznetsov AG, Browning CF, Feldkamp MD, Frank AO, Gilston BA, Olejniczak ET, Rossanese OW, Waterson AG, Chazin WJ, Fesik SW. Identification and Optimization of Anthranilic Acid Based Inhibitors of Replication Protein A. ChemMedChem. 2016. doi: 10.1002/cmdc.201500479. PubMed PMID: 26748787.

Sliwoski G, Schubert M, Stichel J, Weaver D, Beck-Sickinger AG, Meiler J. Discovery of Small-Molecule Modulators of the Human Y4 Receptor. PLoS One. 2016;11(6):e0157146. doi: 10.1371/journal.pone.0157146. PubMed PMID: 27294784.

Swale DR, Engers DW, Bollinger SR, Gross A, Inocente EA, Days E, Kanga F, Johnson RM, Yang L, Bloomquist JR, Hopkins CR, Piermarini PM, Denton JS. An insecticide resistance-breaking mosquitocide targeting inward rectifier potassium channels in vectors of Zika virus and malaria. Sci Rep. 2016;6:36954. doi: 10.1038/srep36954. PubMed PMID: 27849039; PMCID: 5111108.

Swale DR, Kurata H, Kharade SV, Sheehan J, Raphemot R, Voigtritter KR, Figueroa EE, Meiler J, Blobaum AL, Lindsley CW, Hopkins CR, Denton JS. ML418: The First Selective, Sub-Micromolar Pore Blocker of Kir7.1 Potassium Channels. ACS Chem Neurosci. 2016;7(7):1013-23. doi: 10.1021/acschemneuro.6b00111. PubMed PMID: 27184474; PMCID: 5131535.

Trads JB, Burgstaller J, Laprell L, Konrad DB, de la Osa de la Rosa L, Weaver CD, Baier H, Trauner D, Barber DM. Optical control of GIRK channels using visible light. Org Biomol Chem. 2016;15(1):76-81. doi: 10.1039/c6ob02153k. PubMed PMID: 27901161.

Blobaum AL, Byers FW, Bridges TM, Locuson CW, Conn PJ, Lindsley CW, Daniels JS. A Screen of Approved Drugs Identifies the Androgen Receptor Antagonist, Flutamide, and its Pharmacologically Active Metabolite, 2-Hydroxy-Flutamide, as Heterotropic Activators of CYP 3A In vitro and In vivo. Drug Metab Dispos. 2015. doi: 10.1124/dmd.115.064006. PubMed PMID: 26265743.

Conde-Ceide S, Martinez-Viturro CM, Alcazar J, Garcia-Barrantes PM, Lavreysen H, Mackie C, Vinson PN, Rook JM, Bridges TM, Daniels JS, Megens A, Langlois X, Drinkenburg WH, Ahnaou A, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Bartolome-Nebreda JM, Lindsley CW. Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia. ACS Med Chem Lett. 2015;6(6):716-20. doi: 10.1021/acsmedchemlett.5b00181. PubMed PMID: 26157544; PMCID: 4492464.

Du Y, Days E, Romaine I, Abney KK, Kaufmann K, Sulikowski G, Stauffer S, Lindsley CW, Weaver CD. Development and validation of a thallium flux-based functional assay for the sodium channel NaV1.7 and its utility for lead discovery and compound profiling. ACS Chem Neurosci. 2015;6(6):871-8. doi: 10.1021/acschemneuro.5b00004. PubMed PMID: 25879403.

Ghamari-Langroudi M, Digby GJ, Sebag JA, Millhauser GL, Palomino R, Matthews R, Gillyard T, Panaro BL, Tough IR, Cox HM, Denton JS, Cone RD. G-protein-independent coupling of MC4R to Kir7.1 in hypothalamic neurons. Nature. 2015. doi: 10.1038/nature14051. PubMed PMID: 25600267.

Halambage UD, Wong JP, Melancon BJ, Lindsley CW, Aiken C. Microplate-based assay for identifying small molecules that bind a specific intersubunit interface within the assembled HIV-1 capsid. Antimicrob Agents Chemother. 2015;59(9):5190-5. doi: 10.1128/AAC.00646-15. PubMed PMID: 26077250; PMCID: 4538492.

Herington JL, Swale DR, Brown N, Shelton EL, Choi H, Williams CH, Hong CC, Paria BC, Denton JS, Reese J. High-Throughput Screening of Myometrial Calcium-Mobilization to Identify Modulators of Uterine Contractility. PLoS One. 2015;10(11):e0143243. doi: 10.1371/journal.pone.0143243. PubMed PMID: 26600013.

Hill AA, Anderson-Baucum EK, Kennedy AJ, Webb CD, Yull FE, Hasty AH. Activation of NF-κB drives the enhanced survival of adipose tissue macrophages in an obesogenic environment. Molecular Metabolism. 2015;4(10):665-77. doi: 10.1016/j.molmet.2015.07.005.

Kavanaugh G, Zhao R, Guo Y, Mohni KN, Glick G, Lacy ME, Hutson MS, Ascano M, Cortez D. Enhancer of Rudimentary Homolog Affects the Replication Stress Response through Regulation of RNA Processing. Mol Cell Biol. 2015;35(17):2979-90. doi: 10.1128/MCB.01276-14. PubMed PMID: 26100022; PMCID: 4525316.

Mainou BA, Ashbrook AW, Smith EC, Dorset DC, Denison MR, Dermody TS. Serotonin Receptor Agonist 5-Nonyloxytryptamine Alters the Kinetics of Reovirus Cell Entry. J Virol. 2015;89(17):8701-12. doi: 10.1128/JVI.00739-15. PubMed PMID: 26109733; PMCID: 4524060.

Schulte ML, Dawson ES, Saleh SA, Cuthbertson ML, Manning HC. 2-Substituted Ngamma-glutamylanilides as novel probes of ASCT2 with improved potency. Bioorg Med Chem Lett. 2015;25(1):113-6. doi: 10.1016/j.bmcl.2014.10.098. PubMed PMID: 25435145; PMCID: 4372298.

Schulte ML, Khodadadi AB, Cuthbertson ML, Smith JA, Manning HC. 2-Amino-4-bis(aryloxybenzyl)aminobutanoic acids: A novel scaffold for inhibition of ASCT2-mediated glutamine transport. Bioorg Med Chem Lett. 2015. doi: 10.1016/j.bmcl.2015.12.031. PubMed PMID: 26750251.

Skrypnyk NI, Sanker S, Brilli-Skvarca L, Novitskaya T, Woods C, Chiba T, Patel K, Goldberg ND, McDermott L, Vinson PN, Calcutt MW, Huryn DM, Vernetti LA, Vogt A, Hukriede N, de Caestecker MP. Delayed treatment with PTBA analogs reduces post injury renal fibrosis after kidney injury. Am J Physiol Renal Physiol. 2015:ajprenal 00503 2015. doi: 10.1152/ajprenal.00503.2015. PubMed PMID: 26661656.

Smith SA, Silva LA, Fox JM, Flyak AI, Kose N, Sapparapu G, Khomandiak S, Ashbrook AW, Kahle KM, Fong RH, Swayne S, Doranz BJ, McGee CE, Heise MT, Pal P, Brien JD, Austin SK, Diamond MS, Dermody TS, Crowe JE, Jr. Isolation and Characterization of Broad and Ultrapotent Human Monoclonal Antibodies with Therapeutic Activity against Chikungunya Virus. Cell Host Microbe. 2015;18(1):86-95. doi: 10.1016/j.chom.2015.06.009. PubMed PMID: 26159721; PMCID: 4501771.

Zurawski Z, Rodriguez S, Hyde K, Alford S, Hamm H. Gbetagamma binds to the extreme C-terminus of SNAP25 to mediate the action of Gi/o-coupled GPCRs. Mol Pharmacol. 2015. doi: 10.1124/mol.115.101600. PubMed PMID: 26519224.

Burns MC, Sun Q, Daniels RN, Camper D, Kennedy JP, Phan J, Olejniczak ET, Lee T, Waterson AG, Rossanese OW, Fesik SW. Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange. Proc Natl Acad Sci U S A. 2014;111(9):3401-6. doi: 10.1073/pnas.1315798111. PubMed PMID: 24550516; PMCID: 3948241.

Frank AO, Vangamudi B, Feldkamp MD, Souza-Fagundes EM, Luzwick JW, Cortez D, Olejniczak ET, Waterson AG, Rossanese OW, Chazin WJ, Fesik SW. Discovery of a Potent Stapled Helix Peptide That Binds to the 70N Domain of Replication Protein A. J Med Chem. 2014;57(6):2455-61. doi: 10.1021/jm401730y. PubMed PMID: 24491171; PMCID: 3969094.

Kumar KK, Lowe EW, Jr., Aboud AA, Neely MD, Redha R, Bauer JA, Odak M, Weaver CD, Meiler J, Aschner M, Bowman AB. Cellular manganese content is developmentally regulated in human dopaminergic neurons. Sci Rep. 2014;4:6801. doi: 10.1038/srep06801. PubMed PMID: 25348053; PMCID: 4210885.

Morris LC, Days EL, Turney M, Mi D, Lindsley CW, Weaver CD, Niswender KD. A Duplexed High-Throughput Screen to Identify Allosteric Modulators of the Glucagon-Like Peptide 1 and Glucagon Receptors. J Biomol Screen. 2014. doi: 10.1177/1087057114520971. PubMed PMID: 24525870.

Morris LC, Nance KD, Gentry PR, Days EL, Weaver CD, Niswender CM, Thompson AD, Jones CK, Locuson CW, Morrison RD, Daniels JS, Niswender KD, Lindsley CW. Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-py rrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM). J Med Chem. 2014;57(23):10192-7. doi: 10.1021/jm501375c. PubMed PMID: 25423411; PMCID: 4266362.

Raphemot R, Rouhier MF, Swale DR, Days E, Weaver CD, Lovell KM, Konkel LC, Engers DW, Bollinger SR, Hopkins C, Piermarini PM, Denton JS. Discovery and characterization of a potent and selective inhibitor of Aedes aegypti inward rectifier potassium channels. PLoS One. 2014;9(11):e110772. doi: 10.1371/journal.pone.0110772. PubMed PMID: 25375326; PMCID: 4222822.

Raphemot R, Swale DR, Dadi PK, Jacobson DA, Cooper P, Wojtovich AP, Banerjee S, Nichols CG, Denton JS. Direct Activation of beta-Cell KATP Channels with a Novel Xanthine Derivative. Mol Pharmacol. 2014;85(6):858-65. doi: 10.1124/mol.114.091884. PubMed PMID: 24646456.

Sandlin RD, Fong KY, Wicht KJ, Carrell HM, Egan TJ, Wright DW. Identification of beta-hematin inhibitors in a high-throughput screening effort reveals scaffolds with in vitro antimalarial activity. Int J Parasitol Drugs Drug Resist. 2014;4(3):316-25. doi: 10.1016/j.ijpddr.2014.08.002. PubMed PMID: 25516843; PMCID: 4266794.

Sugitani N, Shell SM, Soss SE, Chazin WJ. Redefining the DNA-binding domain of human XPA. J Am Chem Soc. 2014;136(31):10830-3. doi: 10.1021/ja503020f. PubMed PMID: 25056193; PMCID: 4132956.

Wen W, Wu W, Weaver CD, Lindsley CW. Discovery of potent and selective GIRK1/2 modulators via 'molecular switches' within a series of 1-(3-cyclopropyl-1-phenyl-1H-pyrazol-5-yl)ureas. Bioorg Med Chem Lett. 2014;24(21):5102-6. doi: 10.1016/j.bmcl.2014.08.061. PubMed PMID: 25264075.

Wen W, Young SE, Duvernay MT, Schulte ML, Nance KD, Melancon BJ, Engers J, Locuson CW, 2nd, Wood MR, Daniels JS, Wu W, Lindsley CW, Hamm HE, Stauffer SR. Substituted indoles as selective protease-activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354. Bioorg Med Chem Lett. 2014;24(19):4708-13. doi: 10.1016/j.bmcl.2014.08.021. PubMed PMID: 25176330.

Butkiewicz M, Lowe EW, Mueller R, Mendenhall JL, Teixeira PL, Weaver CD, Meiler J. Benchmarking Ligand-Based Virtual High-Throughput Screening with the PubChem Database. Molecules. 2013;18(1):735-56. doi: 10.3390/molecules18010735. PubMed PMID: 23299552.

Feldkamp MD, Frank AO, Kennedy JP, Patrone JD, Vangamudi B, Waterson AG, Fesik SW, Chazin WJ. Surface reengineering of RPA70N enables cocrystallization with an inhibitor of the replication protein A interaction motif of ATR interacting protein. Biochemistry. 2013;52(37):6515-24. doi: 10.1021/bi400542z. PubMed PMID: 23962067; PMCID: 3804075.

Frank AO, Feldkamp MD, Kennedy JP, Waterson AG, Pelz NF, Patrone JD, Vangamudi B, Camper DV, Rossanese OW, Chazin WJ, Fesik SW. Discovery of a potent inhibitor of replication protein a protein-protein interactions using a fragment-linking approach. J Med Chem. 2013;56(22):9242-50. doi: 10.1021/jm401333u. PubMed PMID: 24147804.

Friberg A, Vigil D, Zhao B, Daniels RN, Burke JP, Garcia-Barrantes PM, Camper D, Chauder BA, Lee T, Olejniczak ET, Fesik SW. Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design. J Med Chem. 2013;56(1):15-30. doi: 10.1021/jm301448p. PubMed PMID: 23244564; PMCID: 3646517.

Kaufmann K, Romaine I, Days E, Pascual C, Malik A, Yang L, Zou B, Du Y, Sliwoski G, Morrison RD, Denton J, Niswender CM, Daniels JS, Sulikowski GA, Xie XS, Lindsley CW, Weaver CD. ML297 (VU0456810), the First Potent and Selective Activator of the GIRK Potassium Channel, Displays Antiepileptic Properties in Mice. ACS Chem Neurosci. 2013. doi: 10.1021/cn400062a. PubMed PMID: 23730969.

Mainou BA, Zamora PF, Ashbrook AW, Dorset DC, Kim KS, Dermody TS. Reovirus cell entry requires functional microtubules. MBio. 2013;4(4). doi: 10.1128/mBio.00405-13. PubMed PMID: 23820395; PMCID: 3705452.

Mike LA, Dutter BF, Stauff DL, Moore JL, Vitko NP, Aranmolate O, Kehl-Fie TE, Sullivan S, Reid PR, DuBois JL, Richardson AR, Caprioli RM, Sulikowski GA, Skaar EP. Activation of heme biosynthesis by a small molecule that is toxic to fermenting Staphylococcus aureus. Proc Natl Acad Sci U S A. 2013;110(20):8206-11. doi: 10.1073/pnas.1303674110. PubMed PMID: 23630262; PMCID: 3657828.

Patrone JD, Kennedy JP, Frank AO, Feldkamp MD, Vangamudi B, Pelz NF, Rossanese OW, Waterson AG, Chazin WJ, Fesik SW. Discovery of Protein-Protein Interaction Inhibitors of Replication Protein A. ACS Med Chem Lett. 2013;4(7):601-5. doi: 10.1021/ml400032y. PubMed PMID: 23914285; PMCID: 3728914.

Ramos-Hunter SJ, Engers DW, Kaufmann K, Du Y, Lindsley CW, Weaver CD, Sulikowski GA. Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators. Bioorg Med Chem Lett. 2013;23(18):5195-8. doi: 10.1016/j.bmcl.2013.07.002. PubMed PMID: 23916258; PMCID: 4066871.

Raphemot R, Kadakia RJ, Olsen ML, Banerjee S, Days E, Smith SS, Weaver CD, Denton JS. Development and validation of fluorescence-based and automated patch clamp-based functional assays for the inward rectifier potassium channel Kir4.1. Assay Drug Dev Technol. 2013;11(9-10):532-43. doi: 10.1089/adt.2013.544. PubMed PMID: 24266659; PMCID: 3870600.

Raphemot R, Rouhier MF, Hopkins CR, Gogliotti RD, Lovell KM, Hine RM, Ghosalkar D, Longo A, Beyenbach KW, Denton JS, Piermarini PM. Eliciting renal failure in mosquitoes with a small-molecule inhibitor of inward-rectifying potassium channels. PLoS One. 2013;8(5):e64905. doi: 10.1371/journal.pone.0064905. PubMed PMID: 23734226; PMCID: 3666979.

Raphemot R, Weaver CD, Denton JS. High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels. J Vis Exp. 2013(71). doi: 10.3791/4209. PubMed PMID: 23381507.

Shell SM, Hawkins EK, Tsai M-S, Hlaing AS, Rizzo CJ, Chazin WJ. Xeroderma pigmentosum complementation group C protein (XPC) serves as a general sensor of damaged DNA. DNA Repair. 2013;12(11):947-53. doi: http://dx.doi.org/10.1016/j.dnarep.2013.08.013.

Xie J, Wang C, Virostko J, Manning HC, Pham W, Bauer J, Gore JC. A novel reporter system for molecular imaging and high-throughput screening of anticancer drugs. Chembiochem. 2013;14(12):1494-503. doi: 10.1002/cbic.201300142. PubMed PMID: 23881799; PMCID: 3819221.

Young SE, Duvernay MT, Schulte ML, Lindsley CW, Hamm HE. Synthesis of indole derived protease-activated receptor 4 antagonists and characterization in human platelets. PLoS One. 2013;8(6):e65528. doi: 10.1371/journal.pone.0065528. PubMed PMID: 23776495; PMCID: 3679140.

Blattermann S, Peters L, Ottersbach PA, Bock A, Konya V, Weaver CD, Gonzalez A, Schroder R, Tyagi R, Luschnig P, Gab J, Hennen S, Ulven T, Pardo L, Mohr K, Gutschow M, Heinemann A, Kostenis E. A biased ligand for OXE-R uncouples Galpha and Gbetagamma signaling within a heterotrimer. Nat Chem Biol. 2012;8(7):631-8. doi: 10.1038/nchembio.962. PubMed PMID: 22634634.

Delpire E, Baranczak A, Waterson AG, Kim K, Kett N, Morrison RD, Daniels JS, Weaver CD, Lindsley CW. Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe. Bioorg Med Chem Lett. 2012;22(14):4532-5. doi: 10.1016/j.bmcl.2012.05.126. PubMed PMID: 22727639; PMCID: 3389279.

Jones PL, Pask GM, Romaine IM, Taylor RW, Reid PR, Waterson AG, Sulikowski GA, Zwiebel LJ. Allosteric Antagonism of Insect Odorant Receptor Ion Channels. PLoS ONE. 2012;7(1):e30304. doi: 10.1371/journal.pone.0030304.

Mueller R, Dawson ES, Niswender CM, Butkiewicz M, Hopkins CR, Weaver CD, Lindsley CW, Conn PJ, Meiler J. Iterative experimental and virtual high-throughput screening identifies metabotropic glutamate receptor subtype 4 positive allosteric modulators. J Mol Model. 2012;18(9):4437-46. doi: 10.1007/s00894-012-1441-0. PubMed PMID: 22592386; PMCID: 3766737.

Noetzel MJ, Rook JM, Vinson PN, Cho HP, Days E, Zhou Y, Rodriguez AL, Lavreysen H, Stauffer SR, Niswender CM, Xiang Z, Daniels JS, Jones CK, Lindsley CW, Weaver CD, Conn PJ. Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function. Mol Pharmacol. 2012;81(2):120-33. doi: 10.1124/mol.111.075184. PubMed PMID: 22021324; PMCID: 3263948.

Potet F, Lorinc AN, Chaigne S, Hopkins CR, Venkataraman R, Stepanovic SZ, Lewis LM, Days E, Sidorov VY, Engers DW, Zou B, Afshartous D, George AL, Campbell CM, Balser JR, Li M, Baudenbacher FJ, Lindsley CW, Weaver CD, Kupershmidt S. Identification and Characterization of a Compound That Protects Cardiac Tissue from Human Ether-à-go-go-related Gene (hERG)-related Drug-induced Arrhythmias. Journal of Biological Chemistry. 2012;287(47):39613-25. doi: 10.1074/jbc.M112.380162.

Rinker DC, Jones PL, Pitts RJ, Rutzler M, Camp G, Sun L, Xu P, Dorset DC, Weaver D, Zwiebel LJ. Novel high-throughput screens of Anopheles gambiae odorant receptors reveal candidate behaviour-modifying chemicals for mosquitoes. Physiological Entomology. 2012;37(1):33-41. doi: 10.1111/j.1365-3032.2011.00821.x.

Ruggiero AM, Wright J, Ferguson SM, Lewis M, Emerson KS, Iwamoto H, Ivy MT, Holmstrand EC, Ennis EA, Weaver CD, Blakely RD. Nonoisotopic Assay for the Presynaptic Choline Transporter Reveals Capacity for Allosteric Modulation of Choline Uptake. ACS Chemical Neuroscience. 2012;3(10):767-81. doi: 10.1021/cn3000718.

Souza-Fagundes EM, Frank AO, Feldkamp MD, Dorset DC, Chazin WJ, Rossanese OW, Olejniczak ET, Fesik SW. A high-throughput fluorescence polarization anisotropy assay for the 70N domain of replication protein A. Anal Biochem. 2012;421(2):742-9. doi: 10.1016/j.ab.2011.11.025. PubMed PMID: 22197419; PMCID: 3274598.

Sun Q, Burke JP, Phan J, Burns MC, Olejniczak ET, Waterson AG, Lee T, Rossanese OW, Fesik SW. Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation. Angew Chem Int Ed Engl. 2012;51(25):6140-3. doi: 10.1002/anie.201201358. PubMed PMID: 22566140; PMCID: 3620661.

Bhave G, Chauder BA, Liu W, Dawson ES, Kadakia R, Nguyen TT, Lewis LM, Meiler J, Weaver CD, Satlin LM, Lindsley CW, Denton JS. Development of a selective small-molecule inhibitor of Kir1.1, the renal outer medullary potassium channel. Mol Pharmacol. 2011;79(1):42-50. doi: 10.1124/mol.110.066928. PubMed PMID: 20926757; PMCID: 3014278.

Cheung YY, Zamorano R, Blobaum AL, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu(4). ACS Comb Sci. 2011;13(2):159-65. doi: 10.1021/co1000508. PubMed PMID: 21338051; PMCID: 3057427.

Engers DW, Field JR, Le U, Zhou Y, Bolinger JD, Zamorano R, Blobaum AL, Jones CK, Jadhav S, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats. J Med Chem. 2011;54(4):1106-10. doi: 10.1021/jm101271s. PubMed PMID: 21247167; PMCID: 3166797.

Jones CK, Engers DW, Thompson AD, Field JR, Blobaum AL, Lindsley SR, Zhou Y, Gogliotti RD, Jadhav S, Zamorano R, Bogenpohl J, Smith Y, Morrison R, Daniels JS, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkinsonian animal model. J Med Chem. 2011;54(21):7639-47. doi: 10.1021/jm200956q. PubMed PMID: 21966889; PMCID: 3226828.

Jones PL, Pask GM, Rinker DC, Zwiebel LJ. Functional agonism of insect odorant receptor ion channels. Proc Natl Acad Sci U S A. 2011;108(21):8821-5. doi: 10.1073/pnas.1102425108. PubMed PMID: 21555561; PMCID: 3102409.

Lamb JP, Engers DW, Niswender CM, Rodriguez AL, Venable DF, Conn PJ, Lindsley CW. Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists. Bioorg Med Chem Lett. 2011;21(9):2711-4. doi: 10.1016/j.bmcl.2010.11.119. PubMed PMID: 21183344; PMCID: 3179182.

Lovly CM, Heuckmann JM, de Stanchina E, Chen H, Thomas RK, Liang C, Pao W. Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinase inhibitors. Cancer Res. 2011;71(14):4920-31. doi: 10.1158/0008-5472.CAN-10-3879. PubMed PMID: 21613408; PMCID: 3138877.

Manna JD, Reyzer ML, Latham JC, Weaver CD, Marnett LJ, Caprioli RM. High-throughput quantification of bioactive lipids by MALDI mass spectrometry: application to prostaglandins. Anal Chem. 2011;83(17):6683-8. doi: 10.1021/ac201224n. PubMed PMID: 21770391; PMCID: 3165080.

Pantel J, Williams SY, Mi D, Sebag J, Corbin JD, Weaver CD, Cone RD. Development of a high-throughput screen for allosteric modulators of melanocortin-4 receptor signaling using a real-time cAMP assay. European Journal of Pharmacology. 2011;660(1):139-47. doi: http://dx.doi.org/10.1016/j.ejphar.2011.01.031.

Raphemot R, Lonergan DF, Nguyen TT, Utley T, Lewis LM, Kadakia R, Weaver CD, Gogliotti R, Hopkins C, Lindsley CW, Denton JS. Discovery, characterization, and structure-activity relationships of an inhibitor of inward rectifier potassium (Kir) channels with preference for Kir2.3, Kir3.x, and Kir7.1. Front Pharmacol. 2011;2:75. doi: 10.3389/fphar.2011.00075. PubMed PMID: 22275899; PMCID: 3254186.

Reid PR, Bridges TM, Sheffler DJ, Cho HP, Lewis LM, Days E, Daniels JS, Jones CK, Niswender CM, Weaver CD, Conn PJ, Lindsley CW, Wood MR. Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): The development of ML169, an MLPCN probe. Bioorganic & Medicinal Chemistry Letters. 2011;21(9):2697-701. doi: http://dx.doi.org/10.1016/j.bmcl.2010.12.015.

Sandlin RD, Carter MD, Lee PJ, Auschwitz JM, Leed SE, Johnson JD, Wright DW. Use of the NP-40 detergent-mediated assay in discovery of inhibitors of beta-hematin crystallization. Antimicrob Agents Chemother. 2011;55(7):3363-9. doi: 10.1128/AAC.00121-11. PubMed PMID: 21518844; PMCID: 3122397.

Stoops SL, Pearson AS, Weaver C, Waterson AG, Days E, Farmer C, Brady S, Weaver CD, Beauchamp RD, Lindsley CW. Identification and Optimization of Small Molecules That Restore E-Cadherin Expression and Reduce Invasion in Colorectal Carcinoma Cells. ACS Chemical Biology. 2011;6(5):452-65. doi: 10.1021/cb100305h.

Thorne CA, Lafleur B, Lewis M, Hanson AJ, Jernigan KK, Weaver DC, Huppert KA, Chen TW, Wichaidit C, Cselenyi CS, Tahinci E, Meyers KC, Waskow E, Orton D, Salic A, Lee LA, Robbins DJ, Huppert SS, Lee E. A biochemical screen for identification of small-molecule regulators of the Wnt pathway using Xenopus egg extracts. J Biomol Screen. 2011;16(9):995-1006. doi: 10.1177/1087057111416657. PubMed PMID: 21859680; PMCID: 3694444.

Williams R, Manka JT, Rodriguez AL, Vinson PN, Niswender CM, Weaver CD, Jones CK, Conn PJ, Lindsley CW, Stauffer SR. Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold. Bioorg Med Chem Lett. 2011;21(5):1350-3. doi: 10.1016/j.bmcl.2011.01.044. PubMed PMID: 21315585; PMCID: 3498823.

Wilson AJ, Holson E, Wagner F, Zhang YL, Fass DM, Haggarty SJ, Bhaskara S, Hiebert SW, Schreiber SL, Khabele D. The DNA damage mark pH2AX differentiates the cytotoxic effects of small molecule HDAC inhibitors in ovarian cancer cells. Cancer Biol Ther. 2011;12(6):484-93. doi: 10.4161/cbt.12.6.15956. PubMed PMID: 21738006; PMCID: 3218590.

Xiang Z, Thompson AD, Brogan JT, Schulte ML, Melancon BJ, Mi D, Lewis LM, Zou B, Yang L, Morrison R, Santomango T, Byers F, Brewer K, Aldrich JS, Yu H, Dawson ES, Li M, McManus O, Jones CK, Daniels JS, Hopkins CR, Xie XS, Conn PJ, Weaver CD, Lindsley CW. The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease. ACS Chem Neurosci. 2011;2(12):730-42. doi: 10.1021/cn200090z. PubMed PMID: 22368764; PMCID: 3285241.

Bridges TM, Lewis LM, Dawson ES, Weaver CD, Lindsley CW. Discovery and development of the a highly selective M1 Positive Allosteric Modulator (PAM). Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD)2010. PMID: 21433387. Bookshelf ID: NBK50695

Bridges TM, Lewis LM, Weaver CD, Wood MR, Daniels JS, Conn PJ, Lindsley CW. Development of the First Highly Selective mAChR 5 (M5) Positive Allosteric Modulator (PAM). Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD)2010. PMID: 23762960. Bookshelf ID: NBK143193

Bridges TM, Niswender CM, Jones CK, Lewis LM, Weaver CD, Wood MR, Daniels JS, Conn PJ, Lindsley CW. Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity. Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD)2010. PMID: 23762955. Bookshelf ID: NBK143196

Bridges TM, Reid PR, Lewis LM, Dawson ES, Weaver CD, Wood MR, Lindsley CW. Discovery and development of a second highly selective M1 Positive Allosteric Modulator (PAM). Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD)2010. PMID: 21433394. Bookshelf ID: NBK50704

Days E, Kaufmann K, Romaine I, Niswender C, Lewis M, Utley T, Du Y, Sliwoski G, Morrison R, Dawson ES, Engers JL, Denton J, Daniels JS, Sulikowski GA, Lindsley CW, Weaver CD. Discovery and Characterization of a Selective Activator of the G-Protein Activated Inward-Rectifying Potassium (GIRK) Channel. Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD)2010. PMID: 23762945. Bookshelf ID: NBK143539

Denton JS, Weaver CD, Lewis LM, Chauder BA, Lindsley CW. Discovery of a small molecule inhibitor of ROMK and Kir7.1. Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD)2010. PMID: 21433378. Bookshelf ID: NBK50685

Engers DW, Gentry PR, Williams R, Bolinger JD, Weaver CD, Menon UN, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). Bioorg Med Chem Lett. 2010;20(17):5175-8. doi: 10.1016/j.bmcl.2010.07.007. PubMed PMID: 20667732; PMCID: 2922490.

Hammond AS, Rodriguez AL, Townsend SD, Niswender CM, Gregory KJ, Lindsley CW, Conn PJ. Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology. ACS Chem Neurosci. 2010;1(10):702-16. doi: 10.1021/cn100051m. PubMed PMID: 20981342; PMCID: 2957851.

Hopkins CR, Engers DW, Niswender CM, Jones CK, Dawson E, Weaver CD, Daniels JS, Conn PJ, Lindsley CW. Discovery of a potent, selective and orally active in vivo mGlu4 positive allosteric modulator. Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD)2010. PMID: 23762961. Bookshelf ID: NBK143194

Hopkins CR, Niswender CM, Lewis LM, Weaver CD, Lindsley CW. Discovery of a potent, selective and in vivo active mGluR4 positive allosteric modulator. Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD)2010. PMID: 21433377. Bookshelf ID: NBK50684

Lebois EP, Bridges TM, Lewis LM, Dawson ES, Kane AS, Xiang Z, Jadhav SB, Yin H, Kennedy JP, Meiler J, Niswender CM, Jones CK, Conn PJ, Weaver CD, Lindsley CW. Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system. ACS Chem Neurosci. 2010;1(2):104-21. doi: 10.1021/cn900003h. PubMed PMID: 21961051; PMCID: 3180826.

Lewis LM, Bridges TM, Niswender CM, Weaver CD, Lindsley CW. Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator (PAM). Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD)2010. PMID: 21433380. Bookshelf ID: NBK50687

Lewis M, Weaver CD, McClain MS. Identification of Small Molecule Inhibitors of Clostridium perfringens ε-Toxin Cytotoxicity Using a Cell-Based High-Throughput Screen. Toxins. 2010;2(7):1825-47. PubMed PMID: doi:10.3390/toxins2071825.

Lindsley C, Lewis M, Weaver D. Discovery of a Highly Selective in vitro and in vivo M1 Allosteric Agonist Probe. Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD)2010. PMID: 21433356. Bookshelf ID: NBK47340

Lindsley C, Lewis M, Weaver D, Delpire E. Discovery of a Highly Selective KCC2 Antagonist. Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD)2010. PMID: 21433363. Bookshelf ID: NBK47347

Mueller R, Rodriguez AL, Dawson ES, Butkiewicz M, Nguyen TT, Oleszkiewicz S, Bleckmann A, Weaver CD, Lindsley CW, Conn PJ, Meiler J. Identification of Metabotropic Glutamate Receptor Subtype 5 Potentiators Using Virtual High-Throughput Screening. ACS Chem Neurosci. 2010;1(4):288-305. doi: 10.1021/cn9000389. PubMed PMID: 20414370; PMCID: 2857954.

Niswender CM, Johnson KA, Miller NR, Ayala JE, Luo Q, Williams R, Saleh S, Orton D, Weaver CD, Conn PJ. Context-dependent pharmacology exhibited by negative allosteric modulators of metabotropic glutamate receptor 7. Mol Pharmacol. 2010;77(3):459-68. doi: 10.1124/mol.109.058768. PubMed PMID: 20026717; PMCID: 2835423.

Rodriguez AL, Grier MD, Jones CK, Herman EJ, Kane AS, Smith RL, Williams R, Zhou Y, Marlo JE, Days EL, Blatt TN, Jadhav S, Menon UN, Vinson PN, Rook JM, Stauffer SR, Niswender CM, Lindsley CW, Weaver CD, Conn PJ. Discovery of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Reveals Chemical and Functional Diversity and In Vivo Activity in Rat Behavioral Models of Anxiolytic and Antipsychotic Activity. Molecular Pharmacology. 2010;78(6):1105-23. doi: 10.1124/mol.110.067207.

Rubinson EH, Gowda AS, Spratt TE, Gold B, Eichman BF. An unprecedented nucleic acid capture mechanism for excision of DNA damage. Nature. 2010;468(7322):406-11. doi: 10.1038/nature09428. PubMed PMID: 20927102.

Williams R, Zhou Y, Niswender CM, Luo Q, Conn PJ, Lindsley CW, Hopkins CR. Re-exploration of the PHCCC Scaffold: Discovery of Improved Positive Allosteric Modulators of mGluR4. ACS Chem Neurosci. 2010;1(6):411-9. doi: 10.1021/cn9000318. PubMed PMID: 20582156; PMCID: 2889702.

Xie X, Brogan JT, Schulte ML, Mi D, Yu H, Dawson ES, Li M, McManus O, Engers J, Lewis LM, Thompson A, Jones CK, Weaver CD, Lindsley CW. Scaffold Hopping Affords a Highly Selective in vitro and in vivo T-Type Calcium Inhibitor Probe Free From IP Issues. Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD)2010. PMID: 23762962. Bookshelf ID: NBK143195

Zhou Y, Manka JT, Rodriguez AL, Weaver CD, Days EL, Vinson PN, Jadhav S, Hermann EJ, Jones CK, Conn PJ, Lindsley CW, Stauffer SR. Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity. ACS Med Chem Lett. 2010;1(8):433-8. doi: 10.1021/ml100181a. PubMed PMID: 23308336; PMCID: 3539763.

Bridges TM, Marlo JE, Niswender CM, Jones CK, Jadhav SB, Gentry PR, Plumley HC, Weaver CD, Conn PJ, Lindsley CW. Discovery of the First Highly M5-Preferring Muscarinic Acetylcholine Receptor Ligand, an M5 Positive Allosteric Modulator Derived from a Series of 5-Trifluoromethoxy N-Benzyl Isatins. Journal of Medicinal Chemistry. 2009;52(11):3445-8. doi: 10.1021/jm900286j.

Delpire E, Days E, Lewis LM, Mi D, Kim K, Lindsley CW, Weaver CD. Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2. Proceedings of the National Academy of Sciences. 2009;106(13):5383-8. doi: 10.1073/pnas.0812756106.

Engers DW, Niswender CM, Weaver CD, Jadhav S, Menon UN, Zamorano R, Conn PJ, Lindsley CW, Hopkins CR. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). J Med Chem. 2009;52(14):4115-8. doi: 10.1021/jm9005065. PubMed PMID: 19469556; PMCID: 2765192.

Felts AS, Saleh SA, Le U, Rodriguez AL, Weaver CD, Conn PJ, Lindsley CW, Emmitte KA. Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5. Bioorg Med Chem Lett. 2009;19(23):6623-6. doi: 10.1016/j.bmcl.2009.10.024. PubMed PMID: 19854049; PMCID: 2801349.

Lewis LM, Bhave G, Chauder BA, Banerjee S, Lornsen KA, Redha R, Fallen K, Lindsley CW, Weaver CD, Denton JS. High-Throughput Screening Reveals a Small-Molecule Inhibitor of the Renal Outer Medullary Potassium Channel and Kir7.1. Molecular Pharmacology. 2009;76(5):1094-103. doi: 10.1124/mol.109.059840.

Marlo JE, Niswender CM, Days EL, Bridges TM, Xiang Y, Rodriguez AL, Shirey JK, Brady AE, Nalywajko T, Luo Q, Austin CA, Williams MB, Kim K, Williams R, Orton D, Brown HA, Lindsley CW, Weaver CD, Conn PJ. Discovery and Characterization of Novel Allosteric Potentiators of M1 Muscarinic Receptors Reveals Multiple Modes of Activity. Molecular Pharmacology. 2009;75(3):577-88. doi: 10.1124/mol.108.052886.

Rodriguez AL, Williams R, Zhou Y, Lindsley SR, Le U, Grier MD, Weaver CD, Conn PJ, Lindsley CW. Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype. Bioorg Med Chem Lett. 2009;19(12):3209-13. doi: 10.1016/j.bmcl.2009.04.110. PubMed PMID: 19443219; PMCID: 3177605.

Sheffler DJ, Williams R, Bridges TM, Xiang Z, Kane AS, Byun NE, Jadhav S, Mock MM, Zheng F, Lewis LM, Jones CK, Niswender CM, Weaver CD, Lindsley CW, Conn PJ. A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning. Mol Pharmacol. 2009;76(2):356-68. doi: 10.1124/mol.109.056531. PubMed PMID: 19407080; PMCID: 2713127.

Weaver CD, Sheffler DJ, Lewis LM, Bridges TM, Williams R, Nalywajko NT, Kennedy JP, Mulder MM, Jadhav S, Aldrich LA, Jones CK, Marlo JE, Niswender CM, Mock MM, Zheng F, Conn PJ, Lindsley CW. Discovery and development of a potent and highly selective small molecule muscarinic acetylcholine receptor subtype I (mAChR 1 or M1) antagonist in vitro and in vivo probe. Curr Top Med Chem. 2009;9(13):1217-26. DOI: 10.2174/156802609789753635. PubMed PMID: 19807667.

Williams R, Johnson KA, Gentry PR, Niswender CM, Weaver CD, Conn PJ, Lindsley CW, Hopkins CR. Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4). Bioorg Med Chem Lett. 2009;19(17):4967-70. doi: 10.1016/j.bmcl.2009.07.072. PubMed PMID: 19640716; PMCID: 2752865.

Zhou Y, Rodriguez AL, Williams R, Weaver CD, Conn PJ, Lindsley CW. Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS. Bioorg Med Chem Lett. 2009;19(23):6502-6. doi: 10.1016/j.bmcl.2009.10.059. PubMed PMID: 19875287; PMCID: 3177597.

Lewis LM, Sheffler D, Williams R, Bridges TM, Kennedy JP, Brogan JT, Mulder MJ, Williams L, Nalywajko NT, Niswender CM, Weaver CD, Conn PJ, Lindsley CW. Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists. Bioorg Med Chem Lett. 2008;18(3):885-90. doi: 10.1016/j.bmcl.2007.12.051. PubMed PMID: 18178088; PMCID: 2275053.

Niswender CM, Johnson KA, Luo Q, Ayala JE, Kim C, Conn PJ, Weaver CD. A novel assay of Gi/o-linked G protein-coupled receptor coupling to potassium channels provides new insights into the pharmacology of the group III metabotropic glutamate receptors. Mol Pharmacol. 2008;73(4):1213-24. doi: 10.1124/mol.107.041053. PubMed PMID: 18171729.

Niswender CM, Johnson KA, Weaver CD, Jones CK, Xiang Z, Luo Q, Rodriguez AL, Marlo JE, de Paulis T, Thompson AD, Days EL, Nalywajko T, Austin CA, Williams MB, Ayala JE, Williams R, Lindsley CW, Conn PJ. Discovery, Characterization, and Antiparkinsonian Effect of Novel Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4. Molecular Pharmacology. 2008;74(5):1345-58. doi: 10.1124/mol.108.049551.

Shirey JK, Xiang Z, Orton D, Brady AE, Johnson KA, Williams R, Ayala JE, Rodriguez AL, Wess J, Weaver D, Niswender CM, Conn PJ. An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission. Nat Chem Biol. 2008;4(1):42-50. doi: http://www.nature.com/nchembio/journal/v4/n1/suppinfo/nchembio.2007.55_S1.html.