XY028-140 is a Selective CDK4 and CDK6 PROTAC Degrader
CDKs (Cyclin-dependent kinases) are the families of protein kinases first discovered for their role in regulating the cell cycle. By definition, a CDK binds a regulatory protein called a cyclin. Without cyclin, CDK has little kinase activity; only the cyclin-CDK complex is an active kinase. The four major mechanisms...
Trilaciclib is an Orally Active CDK4 and CDK6 Inhibitor
The cell cycle is a highly conserved process. Additionally, this process must maintain genomic integrity and replicative capacity for proper cell maintenance and proliferation. The cell cycle consists of four distinct phases: G1 or Gap1 phase, G2 or Gap2 phase, and M phase. As we all know, the G1...
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...