• Ma Y, Wang L, Neitzel LR, Loganathan S, Tang N, Qin L, Emily CE, Guo Y, Knapp S, Beauchamp RD, Lee E, Wang J. The MAPK pathway regulates intrinsic resistance to BET inhibitors in colorectal cancer. Clinical cancer research : an official journal of the American Association for Cancer Research. 2016 Sep 27. PMID: 27678457 [PubMed].


The bromodomain and extra-terminal domain (BET) family proteins are epigenetic readers for acetylated histone marks. Emerging BET bromodomain inhibitors have exhibited antineoplastic activities in a wide range of human cancers through suppression of oncogenic transcription factors, including MYC. However, the preclinical activities of BET inhibitors in advanced solid cancers are moderate at best. To improve BET-targeted therapy, we interrogated mechanisms mediating resistance to BET inhibitors in colorectal cancer (CRC).