Fragment-based screening of programmed death ligand 1 (PD-L1) [electronic resource]

• Ngôn ngữ: eng
• Ký hiệu phân loại: 620.19 Other engineering materials
• Thông tin xuất bản: Washington, D.C. : Oak Ridge, Tenn. : United States. Dept. of Energy. Office of Science ; Distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy, 2019
• Mô tả vật lý: Size: p. 786-790 : , digital, PDF file.
• Bộ sưu tập: Metadata
• ID: 260081
• Chủ đề: 1. 60 applied life sciences; 2. Cancer drug discovery; 3. Fragment-based screening; 4. Immunotherapy; 5. Pd-l1 inhibitor; 6. Structure-based design

Tóm tắt

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.