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ID: ALA4422676

Journal: Bioorg Med Chem Lett

Title: Fragment-based screening of programmed death ligand 1 (PD-L1).

Authors: Perry E, Mills JJ, Zhao B, Wang F, Sun Q, Christov PP, Tarr JC, Rietz TA, Olejniczak ET, Lee T, Fesik S.

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.

CiteXplore: 30728114

DOI: 10.1016/j.bmcl.2019.01.028