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1r78

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[[Image:1r78.jpg|left|200px]]
[[Image:1r78.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1r78 |SIZE=350|CAPTION= <scene name='initialview01'>1r78</scene>, resolution 2.00&Aring;
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The line below this paragraph, containing "STRUCTURE_1r78", creates the "Structure Box" on the page.
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|SITE=
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|LIGAND= <scene name='pdbligand=FMD:4-((3R,4S,5R)-4-AMINO-3,5-DIHYDROXY-HEX-1-YNYL)-5-FLUORO-3-[1-(3-METHOXY-1H-PYRROL-2-YL)-METH-(Z)-YLIDENE]-1,3-DIHYDRO-INDOL-2-ONE'>FMD</scene>
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|ACTIVITY=
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|GENE= CDK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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|DOMAIN=
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{{STRUCTURE_1r78| PDB=1r78 | SCENE= }}
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|RELATEDENTRY=[[1fvt|1fvt]], [[1p2a|1p2a]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1r78 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1r78 OCA], [http://www.ebi.ac.uk/pdbsum/1r78 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1r78 RCSB]</span>
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}}
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'''CDK2 complex with a 4-alkynyl oxindole inhibitor'''
'''CDK2 complex with a 4-alkynyl oxindole inhibitor'''
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[[Category: Simcox, M E.]]
[[Category: Simcox, M E.]]
[[Category: Thompson, T.]]
[[Category: Thompson, T.]]
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[[Category: cyclin dependent kinase]]
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[[Category: Cyclin dependent kinase]]
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[[Category: oxindole]]
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[[Category: Oxindole]]
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[[Category: serine/threonine protein kinase]]
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[[Category: Serine/threonine protein kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 07:10:08 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:24:15 2008''
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Revision as of 04:10, 3 May 2008

Image:1r78.jpg

Template:STRUCTURE 1r78

CDK2 complex with a 4-alkynyl oxindole inhibitor


Overview

A novel series of oxindole-type inhibitors of CDK2 that have heteroatom substituted alkynyl moieties at their C-4 position is described. These novel 4-alkynyl-substituted inhibitors have superior potency relative to their parent compound in free enzyme and in cell based assays. The crystal structure of CDK2 in complex with one of these analogues was determined and gives insight to their increased potency. The biochemical evaluation of a representative derivative is also described.

About this Structure

1R78 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

A new series of potent oxindole inhibitors of CDK2., Luk KC, Simcox ME, Schutt A, Rowan K, Thompson T, Chen Y, Kammlott U, DePinto W, Dunten P, Dermatakis A, Bioorg Med Chem Lett. 2004 Feb 23;14(4):913-7. PMID:15012993 Page seeded by OCA on Sat May 3 07:10:08 2008

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