Diversity in CDK structural mechanisms of regulation and drug discovery opportunities

Le résumé fourni par la source

Cyclin-dependent kinases (CDKs) are required for progression through the eukaryotic cell cycle and for gene transcription. The recent determination of structures of CDK-containing complexes by cryogenic electron microscopy has significantly enriched our understanding of the diverse mechanisms by which CDKs can be activated and regulated. Recent studies have also highlighted the importance of short linear motifs within CDK substrates and regulators to CDK activity. Aberrant CDK activity is a hallmark of a number of diseases, including cancers, and selective ATP-competitive inhibitors are in clinical use. Herein, we review recent structural insights into CDK activation and regulation and how these insights suggest alternative ways to modulate CDK activity that may lead to molecules with improved selectivity and/or specificity.

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