1r78
From Proteopedia
(New page: 200px<br /> <applet load="1r78" size="450" color="white" frame="true" align="right" spinBox="true" caption="1r78, resolution 2.00Å" /> '''CDK2 complex with a...) |
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| - | [[Image:1r78. | + | [[Image:1r78.jpg|left|200px]]<br /><applet load="1r78" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1r78" size=" | + | |
caption="1r78, resolution 2.00Å" /> | caption="1r78, resolution 2.00Å" /> | ||
'''CDK2 complex with a 4-alkynyl oxindole inhibitor'''<br /> | '''CDK2 complex with a 4-alkynyl oxindole inhibitor'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1R78 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with FMD as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 1R78 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=FMD:'>FMD</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1R78 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: serine/threonine protein kinase]] | [[Category: serine/threonine protein kinase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:47:21 2008'' |
Revision as of 14:47, 15 February 2008
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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 with as ligand. 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
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