An Analysis of the Binding Modes of ATP-Competitive CDK2 Inhibitors as Revealed by X-Ray Structures of Protein-Inhibitor Complexes

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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An Analysis of the Binding Modes of ATP-Competitive CDK2 Inhibitors as Revealed by X-Ray Structures of Protein-Inhibitor Complexes



Anti-Cancer Agents in Medicinal Chemistry, 5(5): 561-573.

Author(s): A. Vulpetti and P Pevarello.

Affiliation: Department of Chemistry, BU-Oncology, Nerviano Medical Sciences, Via Pasteur, 10, 20014 Nerviano(MI), Italy.

Abstract

CDK2 is an attractive target for the design of new therapeutic antitumor agent. Numerous CDK2 inhibitors have been discovered and their crystallographic structures either in complex with CDK2 or CDK2/Cyclin A have been published. This review aims to summarize the publicly available structural characterization of CDK2/(Cyclin A) - ligand complexes and to highlight the similarities among the binding modes of structurally diverse inhibitors.

Keywords:

cyclin-dependent kinase, cdk, x-ray, cell cycle, crystal structure, binding mode, adenine scaffold, adenine mimics.



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Article Details

Volume: 5
Issue Number: 5
First Page: 561
Last Page: 573
Page Count: 13
DOI: 10.2174/1568011054866928
Price: $58
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