Cell cycle regulatory kinases (CDKs, PLKs, Aurora kinases, CHKs)

Cell cycle regulatory kinases are a diverse group of enzymes that orchestrate the progression of cells through the various phases of the cell cycle, including G1, S, G2, and M phases (NIH, 2024). This class primarily includes cyclin-dependent kinases (CDKs), Aurora kinases, Polo-like kinases (PLKs), and checkpoint kinases (CHKs), which work in concert with regulatory subunits called cyclins to ensure genomic integrity (ResearchGate, 2026). In healthy cells, these kinases regulate critical events such as DNA replication and chromosome segregation; however, their dysregulation is a hallmark of cancer, leading to uncontrolled cell proliferation and therapeutic resistance (Frontiers, 2024). Consequently, these kinases have become major therapeutic targets in oncology (NIH, 2025). Several selective inhibitors, such as those targeting CDK4 and CDK6, have been approved for the treatment of hormone receptor-positive breast cancer (EurekAlert, 2025). Other inhibitors targeting CDK2, Aurora kinases, and WEE1 are currently under clinical investigation to expand the utility of cell cycle-targeted therapies across various malignancies (NIH, 2024).

Other names

Cell cycle kinasesMitotic kinasesCyclin-dependent kinasesAurora kinasesPolo-like kinasesCheckpoint kinases

Inhibition of kinase catalytic activity, typically through ATP-competitive binding, leading to cell cycle arrest at specific checkpoints such as G1/S or G2/M (NIH, 2024; ResearchGate, 2026).