1vyz

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[[Image:1vyz.jpg|left|200px]]
[[Image:1vyz.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1vyz |SIZE=350|CAPTION= <scene name='initialview01'>1vyz</scene>, resolution 2.21&Aring;
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The line below this paragraph, containing "STRUCTURE_1vyz", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:N5b+Binding+Site+For+Chain+A'>AC1</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=N5B:N-(5-CYCLOPROPYL-1H-PYRAZOL-3-YL)BENZAMIDE'>N5B</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_1vyz| PDB=1vyz | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1vyz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1vyz OCA], [http://www.ebi.ac.uk/pdbsum/1vyz PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1vyz RCSB]</span>
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}}
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'''STRUCTURE OF CDK2 COMPLEXED WITH PNU-181227'''
'''STRUCTURE OF CDK2 COMPLEXED WITH PNU-181227'''
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[[Category: Vulpetti, A.]]
[[Category: Vulpetti, A.]]
[[Category: Warpehoski, M A.]]
[[Category: Warpehoski, M A.]]
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[[Category: cell division]]
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[[Category: Cell division]]
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[[Category: cyclin]]
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[[Category: Cyclin]]
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[[Category: phosphorylation]]
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[[Category: Phosphorylation]]
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[[Category: protein kinase]]
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[[Category: Protein kinase]]
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[[Category: serine/threonine-protein kinase]]
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[[Category: Serine/threonine-protein kinase]]
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[[Category: transferase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 12:56:04 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:28:56 2008''
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Revision as of 09:56, 3 May 2008

Image:1vyz.jpg

Template:STRUCTURE 1vyz

STRUCTURE OF CDK2 COMPLEXED WITH PNU-181227


Overview

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 > 50%) in a mouse xenograft model at a dose devoid of toxic effects.

About this Structure

1VYZ is a Single protein structure of sequence 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 Page seeded by OCA on Sat May 3 12:56:04 2008

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OCA

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