CDK4 Subfamily Inhibitors

CDK4 and CDK6

The CDK 4 subfamily of cyclin-dependent kinases consists of CDK4 and CDK6, which function interchangeably in most cell types during G₁ phase of the cell cycle. Both CDK4 and CDK6 bind cyclin D, leading to phosphorylation and inactivation of retinoblastoma protein (Rb) and transcription of E2F target genes, which includes those responsible for cell cycle progression.

Cyclin D interacts with the N-terminal lobe of CDK4; however, no conformational change is induced by its binding ...