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Cyclin-dependent kinases (CDKs) are a family of serine/threonine protein kinases that regulate the cell cycle, transcription, and co-transcriptional processes by forming complexes with cyclins. CDK1 drives cells into mitosis; CDK2 is essential for DNA replication; CDK4 (alongside CDK6) controls G1 phase progression; CDK7 is a component of the general transcription factor TFIIH, activating other CDKs and controlling Pol II transcription; CDK9 is part of the positive transcription elongation factor b (P-TEFb), ensuring transcriptional elongation by RNA polymerase II. Dysregulation of CDKs is strongly associated with cancer, as well as other proliferative and transcription-related diseases, making them important therapeutic targets.
Competitive inhibition of ATP binding site. Inhibition of kinase activity, leading to cell cycle arrest. Blockade of transcriptional CDKs, impairing RNA polymerase II function. Downregulation of anti-apoptotic proteins via transcriptional inhibition.
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