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Molecules 2014, 19(9), 14366-14382; https://doi.org/10.3390/molecules190914366

Cyclin-Dependent Kinase Inhibitors as Marketed Anticancer Drugs: Where Are We Now? A Short Survey

1
Institut Curie, UMR CNRS 176, 26 rue d'Ulm, Paris 75005, France
2
Faculté de Pharmacie de Paris, Université Paris Descartes, UMR CNRS 8638, 4 avenue de l'Observatoire, Paris 75006, France
*
Author to whom correspondence should be addressed.
Received: 25 July 2014 / Revised: 26 August 2014 / Accepted: 28 August 2014 / Published: 11 September 2014
(This article belongs to the Special Issue Design and Study of Kinase Inhibitors)
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Abstract

In the early 2000s, the anticancer drug imatinib (Glivec®) appeared on the market, exhibiting a new mode of action by selective kinase inhibition. Consequently, kinases became a validated therapeutic target, paving the way for further developments. Although these kinases have been thoroughly studied, none of the compounds commercialized since then target cyclin-dependent kinases (CDKs). Following a recent and detailed review on the subject by Galons et al., we concentrate our attention on an updated list of compounds under clinical evaluation (phase I/II/III) and discuss their mode of action as ATP-competitive inhibitors. CDK inhibition profiles and clinical development stages are reported for the 14 compounds under clinical evaluation. Also, tentative progress for forthcoming potential ATP non-competitive inhibitors and allosteric inhibitors are briefly described, along with their limitations. View Full-Text
Keywords: CDK; kinase; inhibitor; anticancer; heterocycle; clinical evaluation; ATP-competitive; allosteric site; ATP non-competitive CDK; kinase; inhibitor; anticancer; heterocycle; clinical evaluation; ATP-competitive; allosteric site; ATP non-competitive
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Mariaule, G.; Belmont, P. Cyclin-Dependent Kinase Inhibitors as Marketed Anticancer Drugs: Where Are We Now? A Short Survey. Molecules 2014, 19, 14366-14382.

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