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1ckp

From Proteopedia

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[[Image:1ckp.gif|left|200px]]
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{{Seed}}
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[[Image:1ckp.png|left|200px]]
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{{STRUCTURE_1ckp| PDB=1ckp | SCENE= }}
{{STRUCTURE_1ckp| PDB=1ckp | SCENE= }}
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'''HUMAN CYCLIN DEPENDENT KINASE 2 COMPLEXED WITH THE INHIBITOR PURVALANOL B'''
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===HUMAN CYCLIN DEPENDENT KINASE 2 COMPLEXED WITH THE INHIBITOR PURVALANOL B===
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==Overview==
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Selective protein kinase inhibitors were developed on the basis of the unexpected binding mode of 2,6,9-trisubstituted purines to the adenosine triphosphate-binding site of the human cyclin-dependent kinase 2 (CDK2). By iterating chemical library synthesis and biological screening, potent inhibitors of the human CDK2-cyclin A kinase complex and of Saccharomyces cerevisiae Cdc28p were identified. The structural basis for the binding affinity and selectivity was determined by analysis of a three-dimensional crystal structure of a CDK2-inhibitor complex. The cellular effects of these compounds were characterized in mammalian cells and yeast. In the latter case the effects were characterized on a genome-wide scale by monitoring changes in messenger RNA levels in treated cells with high-density oligonucleotide probe arrays. Purine libraries could provide useful tools for analyzing a variety of signaling and regulatory pathways and may lead to the development of new therapeutics.
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The line below this paragraph, {{ABSTRACT_PUBMED_9677190}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 9677190 is the PubMed ID number.
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{{ABSTRACT_PUBMED_9677190}}
==About this Structure==
==About this Structure==
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[[Category: Phosphorylation]]
[[Category: Phosphorylation]]
[[Category: Protein kinase]]
[[Category: Protein kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 12:50:24 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 20:52:52 2008''

Revision as of 17:52, 30 June 2008

Image:1ckp.png

Template:STRUCTURE 1ckp

HUMAN CYCLIN DEPENDENT KINASE 2 COMPLEXED WITH THE INHIBITOR PURVALANOL B

Template:ABSTRACT PUBMED 9677190

About this Structure

1CKP is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors., Gray NS, Wodicka L, Thunnissen AM, Norman TC, Kwon S, Espinoza FH, Morgan DO, Barnes G, LeClerc S, Meijer L, Kim SH, Lockhart DJ, Schultz PG, Science. 1998 Jul 24;281(5376):533-8. PMID:9677190

Page seeded by OCA on Mon Jun 30 20:52:52 2008

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