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

Perry, Evan, Mills, Jonathan J, Zhao, Bin, Wang, Feng, Sun, Qi, Christov, Plamen P, Tarr, James C, Rietz, Tyson A, Olejniczak, Edward T, Lee, Taekyu and Fesik, Stephen (2019) Fragment-based screening of programmed death ligand 1 (PD-L1). Bioorganic & medicinal chemistry letters, 29 (6). pp. 786-790. ISSN 1464-3405


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.

Item Type: Article
Date Deposited: 28 Mar 2019 00:45
Last Modified: 28 Mar 2019 00:45


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