1vyw

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{{STRUCTURE_1vyw| PDB=1vyw | SCENE= }}
{{STRUCTURE_1vyw| PDB=1vyw | SCENE= }}
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'''STRUCTURE OF CDK2/CYCLIN A WITH PNU-292137'''
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===STRUCTURE OF CDK2/CYCLIN A WITH PNU-292137===
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==Overview==
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Abnormal proliferation mediated by disruption of the normal cell cycle mechanisms is a hallmark of virtually all cancer cells. Compounds targeting complexes between cyclin-dependent kinases (CDK) and cyclins, such as CDK2/cyclin A and CDK2/cyclin E, and inhibiting their kinase activity are regarded as promising antitumor agents to complement the existing therapies. From a high-throughput screening effort, we identified a new class of CDK2/cyclin A/E inhibitors. The hit-to-lead expansion of this class is described. X-ray crystallographic data of early compounds in this series, as well as in vitro testing funneled for rapidly achieving in vivo efficacy, led to a nanomolar inhibitor of CDK2/cyclin A (N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-(2-naphthyl)acetamide (41), PNU-292137, IC50 = 37 nM) with in vivo antitumor activity (TGI &gt; 50%) in a mouse xenograft model at a dose devoid of toxic effects.
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{{ABSTRACT_PUBMED_15189033}}
==About this Structure==
==About this Structure==
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[[Category: Serine/threonine-protein kinase]]
[[Category: Serine/threonine-protein kinase]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 12:55:45 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 14:12:28 2008''

Revision as of 11:12, 28 July 2008

Image:1vyw.png

Template:STRUCTURE 1vyw

STRUCTURE OF CDK2/CYCLIN A WITH PNU-292137

Template:ABSTRACT PUBMED 15189033

About this Structure

1VYW is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding., Pevarello P, Brasca MG, Amici R, Orsini P, Traquandi G, Corti L, Piutti C, Sansonna P, Villa M, Pierce BS, Pulici M, Giordano P, Martina K, Fritzen EL, Nugent RA, Casale E, Cameron A, Ciomei M, Roletto F, Isacchi A, Fogliatto G, Pesenti E, Pastori W, Marsiglio A, Leach KL, Clare PM, Fiorentini F, Varasi M, Vulpetti A, Warpehoski MA, J Med Chem. 2004 Jun 17;47(13):3367-80. PMID:15189033

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