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Cyclin-dependent kinases (CDKs) are a conserved family of serine/threonine protein kinases that play central roles in regulating the eukaryotic cell cycle, transcription, and other essential cellular processes such as metabolism, apoptosis, and neuronal differentiation. CDKs require association with regulatory subunits called cyclins for their enzymatic activity. The binding of a cyclin induces conformational changes in the CDK that enable its activation—often further regulated by phosphorylation at specific threonine residues. Deregulation or hyperactivation of specific cyclins or their partner kinases is implicated in various diseases such as cancer and neurodegenerative diseases. Because they are central regulators of proliferation and survival pathways—and due to their structural conservation—CDKs are major targets for anticancer drug development.
ATP-binding site inhibition
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