Progress with covalent small-molecule kinase inhibitors

Zheng Zhao, Philip E. Bourne

Drug Discovery Today, 2018

doi: 10.1016/j.drudis.2018.01.035

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.