Current Medicinal Chemistry - Anti-Cancer Agents

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

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

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: 5
Year: 2005
Page: [561 - 573]
Pages: 13
DOI: 10.2174/1568011054866928
Price: $58