Tag: CDK6

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...

CP-10 is a Specific PROTAC Degrader of CDK6

CDK6 plays a significant role in cell cycle entrance. However, overexpression of CDK6 correlates to CDK4/6 inhibitor resistance in breast cancer cell lines and patient samples. Moreover, point mutation of CDK6 could possibly result in attenuation of drug binding affinity or hyperactivation of CDK6. Thus, there is an urgent...

BSJ-03-123, a Degrader with Proteome-wide Selectivity for CDK6 (PROTAC)

A study from Matthias Brand reported a novel phthalimide-based degrader BSJ-03-123. This compound exploits protein-interface determinants to achieve proteome-wide selectivity for the degradation of cyclin-dependent kinase 6 (CDK6). Notably, CDK6 degradation targets a selective dependency of acute myeloid leukemia cells. Cyclin-dependent kinases (CDKs) participate in regulating fundamental cellular processes...