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2c68

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Revision as of 14:54, 30 October 2007 by OCA (Talk | contribs)
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Image:2c68.gif

2c68, resolution 1.95Å

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CRYSTAL STRUCTURE OF THE HUMAN CDK2 COMPLEXED WITH THE TRIAZOLOPYRIMIDINE INHIBITOR

Overview

Crystallographic and modelling data, in conjunction with a medicinal, chemistry template-hopping approach, led to the identification of a series, of novel and potent inhibitors of human cyclin-dependent kinase 2 (CDK2), with selectivity over glycogen synthase kinase-3beta (GSK-3beta). One, example had a CDK2 IC(50) of 120 nM and showed selectivity over GSK-3beta, of 167-fold.

About this Structure

2C68 is a [Single protein] structure of sequence from [Homo sapiens] with CT6 as [ligand]. Active as [Transferred entry: 2.7.11.1], with EC number [2.7.1.37]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].

Reference

Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR., Richardson CM, Williamson DS, Parratt MJ, Borgognoni J, Cansfield AD, Dokurno P, Francis GL, Howes R, Moore JD, Murray JB, Robertson A, Surgenor AE, Torrance CJ, Bioorg Med Chem Lett. 2006 Mar 1;16(5):1353-7. Epub 2005 Dec 1. PMID:16325401

Page seeded by OCA on Tue Oct 30 16:59:23 2007

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