Monday, January 15, 2018

Progress with covalent small-molecule kinase inhibitors

Zheng Zhao, Philip E. Bourne
Drug Discovery Today, 2018
With reduced risk of toxicity and high selectivity, covalent small-molecule kinase inhibitors (CSKIs) have emerged rapidly. Through the lens of structural system pharmacology, here we review this rapid progress by considering design strategies and the challenges and opportunities offered by current CSKIs.

Covalent inhibitor design confers activity against both GDP- and GTP-bound forms of KRAS G12C

Matthew L. Condakes, Zhuo Zhang, Derek B. Danahy, Richard R. Moore, Sirish Kaushik Lakkaraju, Xiaoliang Zhuo, Yuka Amako, Robert M. Borzille...