Fragment-based Screening of Programmed Death Ligand 1 (PD-L1);
AUTHORS
Perry
Evan ,
Mills
Jonathan ,
Zhao
Bin ,
Wang
Feng ,
Sun
Qi ,
Christov
Plamen ,
Tarr
James ,
Rietz
Tyson ,
Olejniczak
Edward ,
Lee
Taekyu ,
Fesik
Stephen ,
. Bioorg Med Chem Lett; . 2019 3 15; 29(6). 786-790
- PMID: 30728114 [PubMed].
- PMCID: PMC6474755.
ABSTRACT
The PD-1 immune checkpoint pathway is a highly validated target for cancer immunotherapy. Despite the potential advantages of small molecule inhibitors over antibodies, the discovery of small molecule checkpoint inhibitors has lagged behind. To discover small molecule inhibitors of the PD-1 pathway, we have utilized a fragment-based approach. Small molecules were identified that bind to PD-L1 and crystal structures of these compounds bound to PD-L1 were obtained.
Tags: 2019