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Cancers 2015, 7(1), 179-237;

Targeting Cyclin-Dependent Kinases in Human Cancers: From Small Molecules to Peptide Inhibitors

Institut des Biomolécules Max Mousseron, IBMM-CNRS-UMR5247, 15 Av. Charles Flahault, 34093 Montpellier, France
These authors contributed equally to this work.
Author to whom correspondence should be addressed.
Academic Editor: Jonas Cicenas
Received: 17 December 2014 / Accepted: 12 January 2015 / Published: 23 January 2015
(This article belongs to the Collection Kinases and Cancer)
Full-Text   |   PDF [2383 KB, uploaded 23 January 2015]   |  


Cyclin-dependent kinases (CDK/Cyclins) form a family of heterodimeric kinases that play central roles in regulation of cell cycle progression, transcription and other major biological processes including neuronal differentiation and metabolism. Constitutive or deregulated hyperactivity of these kinases due to amplification, overexpression or mutation of cyclins or CDK, contributes to proliferation of cancer cells, and aberrant activity of these kinases has been reported in a wide variety of human cancers. These kinases therefore constitute biomarkers of proliferation and attractive pharmacological targets for development of anticancer therapeutics. The structural features of several of these kinases have been elucidated and their molecular mechanisms of regulation characterized in depth, providing clues for development of drugs and inhibitors to disrupt their function. However, like most other kinases, they constitute a challenging class of therapeutic targets due to their highly conserved structural features and ATP-binding pocket. Notwithstanding, several classes of inhibitors have been discovered from natural sources, and small molecule derivatives have been synthesized through rational, structure-guided approaches or identified in high throughput screens. The larger part of these inhibitors target ATP pockets, but a growing number of peptides targeting protein/protein interfaces are being proposed, and a small number of compounds targeting allosteric sites have been reported. View Full-Text
Keywords: CDK/Cyclin Kinase; cell cycle; cancer; inhibitor; peptide; small molecule CDK/Cyclin Kinase; cell cycle; cancer; inhibitor; peptide; small molecule

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Peyressatre, M.; Prével, C.; Pellerano, M.; Morris, M.C. Targeting Cyclin-Dependent Kinases in Human Cancers: From Small Molecules to Peptide Inhibitors. Cancers 2015, 7, 179-237.

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