Date published: 2025-9-11

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Cyclin-dependent kinase 2 (CDK2) inhibitors represent a crucial class of chemical compounds in the field of cancer research and therapy due to their significant role in regulating cell cycle progression. CDK2, a serine/threonine kinase, forms complexes with cyclin E or A during the cell cycle's G1/S transition and S phase, respectively. These complexes are essential for the progression of the cell cycle, particularly for DNA replication and the initiation of mitosis. Inhibiting CDK2 activity can lead to cell cycle arrest, thereby preventing the proliferation of cancer cells. The chemical inhibitors of CDK2, such as Roscovitine, Purvalanol A, and Dinaciclib, are designed to bind to the ATP-binding site of CDK2, reducing its kinase activity and hindering the cell cycle's progression. These inhibitors are valuable tools for researchers studying cell cycle regulation.

The specificity and potency of CDK2 inhibitors vary, with some compounds showing high selectivity towards CDK2, while others inhibit multiple CDKs. This variation allows for different approaches in cancer therapy, targeting specific phases of the cell cycle or a broader range of cancer cell types. For example, Flavopiridol and Dinaciclib are known to inhibit several CDKs, including CDK2, offering a more comprehensive approach to halt cancer cell growth.

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