Discovery of TK-642 as a highly potent, selective, orally bioavailable pyrazolopyrazine-based allosteric SHP2 inhibitor

• Автори: Kai Tang (Автор), Shu Wang (Автор), Siqi Feng (Автор), Xinyu Yang (Автор), Yueyang Guo (Автор), Xiangli Ren (Автор), Linyue Bai (Автор), Bin Yu (Автор), Hong-Min Liu (Автор), Yihui Song (Автор)
• Формат: Книга
• Опубліковано: Elsevier, 2024-08-01T00:00:00Z.
• Предмети: article
• Онлайн доступ: Connect to this object online.

Src homology-2-containing protein tyrosine phosphatase 2 (SHP2) is a promising therapeutic target for cancer therapy. In this work, we presented the structure-guided design of 5,6-fused bicyclic allosteric SHP2 inhibitors, leading to the identification of pyrazolopyrazine-based TK-642 as a highly po...