Advances in protein kinase drug discovery through targeting gatekeeper mutations.

Abstract excerpt

INTRODUCTION: Acquired resistance caused by gatekeeper mutations has become a major challenge for approved kinase inhibitors used in the clinic. Consequently, the development of new-generation inhibitors or degraders to overcome clinical resistance has become an important research focus for the field. AREAS COVERED: This review summarizes the common gatekeeper mutations in druggable kinases and the constantly...

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