Cancer therapies based on targeted protein degradation - lessons learned with lenalidomide.

ABSTRACT: For decades, anticancer targeted therapies have been designed to inhibit kinases or other enzyme classes and have profoundly benefited many patients. However, novel approaches are required to target transcription factors, scaffolding proteins and other proteins central to cancer biology that typically lack catalytic activity and have remained mostly recalcitrant to drug development. The selective degradation of target proteins is an attractive approach to expand the druggable proteome, and the selective oestrogen receptor degrader fulvestrant served as an early example of this concept. Following a long and tragic history in the clinic, the immunomodulatory imide drug (IMiD) thalidomide was discovered to exert its therapeutic activity via a novel and unexpected mechanism of action: targetin

SUBMITTER: Jan M 

PROVIDER: S-EPMC8903027 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature