2c69

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{{STRUCTURE_2c69| PDB=2c69 | SCENE= }}
{{STRUCTURE_2c69| PDB=2c69 | SCENE= }}
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'''CRYSTAL STRUCTURE OF THE HUMAN CDK2 COMPLEXED WITH THE TRIAZOLOPYRIMIDINE INHIBITOR'''
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===CRYSTAL STRUCTURE OF THE HUMAN CDK2 COMPLEXED WITH THE TRIAZOLOPYRIMIDINE INHIBITOR===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 16325401 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16325401}}
==About this Structure==
==About this Structure==
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[[Category: Transferase]]
[[Category: Transferase]]
[[Category: Triazolopyrimidine inhibitor]]
[[Category: Triazolopyrimidine inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 21:19:17 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 13:42:17 2008''

Revision as of 10:42, 28 July 2008

Image:2c69.png

Template:STRUCTURE 2c69

CRYSTAL STRUCTURE OF THE HUMAN CDK2 COMPLEXED WITH THE TRIAZOLOPYRIMIDINE INHIBITOR

Template:ABSTRACT PUBMED 16325401

About this Structure

2C69 is a Single protein structure of sequence from Homo sapiens. 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

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