Cyclin-dependent kinase 1 (CDK1) (CDK1)

Cyclin-dependent kinase 1 (CDK1) is a highly conserved serine/threonine protein kinase that serves as a master regulator of the eukaryotic cell cycle. It is uniquely essential for the transition from G2 phase into mitosis, where it forms a catalytic complex with Cyclin B1 to phosphorylate a wide array of substrates involved in nuclear envelope breakdown, chromosome condensation, and spindle assembly (UniProt P06493). In many human malignancies, including breast, lung, and liver cancers, CDK1 is significantly overexpressed, which facilitates rapid and uncontrolled cell division and is often associated with poor clinical outcomes (PubMed: 26073081). Because of its central role in proliferation, CDK1 has been a primary target for small-molecule inhibitors designed to induce cell cycle arrest and subsequent apoptosis in tumor cells (PubMed: 30103306). However, the development of CDK1 inhibitors faces challenges regarding systemic toxicity and the need for high selectivity to avoid affecting normal regenerative tissues like the bone marrow (StatPearls: Cyclin Dependent Kinase Inhibitors).

Other names

CDC2CDC28ACell division control protein 2 homologp34 protein kinaseCDKN1

Inhibition of the kinase activity by competing with ATP for the binding site, thereby preventing the phosphorylation of substrates necessary for the G2/M transition (PubMed: 30103306).