Tag: CDK4

BSJ-03-204 is a Selective Palbociclib-Based CDK4/6 Dual Degrader (PROTAC)

The chimeric proteolytic enzyme (PROTAC) is a heterobifunctional small molecule. Specifically, it is composed of two active domains and an adaptor that can remove specific proteins that are not needed. Besides, PROTAC does not act as a conventional enzyme inhibitor, but by inducing selective intracellular proteolysis. Moreover, PROTAC includes...

BSJ-04-132 is a Selective Ribociclib-Based CDK4 Degrader (PROTAC)

Targeted protein degradation induced by PROTAC has become a new therapeutic strategy in drug development. Besides, PROTAC has two covalently linked protein binding molecules. One can bind E3 ubiquitin ligases and the other can bind to the target protein to be degraded. Moreover, the recruitment of E3 ligase to...