1r78
From Proteopedia
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==Overview== | ==Overview== | ||
| - | A novel series of oxindole-type inhibitors of CDK2 that have heteroatom | + | 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== | ==About this Structure== | ||
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[[Category: Dunten, P.]] | [[Category: Dunten, P.]] | ||
[[Category: Kammlott, U.]] | [[Category: Kammlott, U.]] | ||
| - | [[Category: Luk, K | + | [[Category: Luk, K C.]] |
[[Category: Rowan, K.]] | [[Category: Rowan, K.]] | ||
[[Category: Schutt, A.]] | [[Category: Schutt, A.]] | ||
| - | [[Category: Simcox, M | + | [[Category: Simcox, M E.]] |
[[Category: Thompson, T.]] | [[Category: Thompson, T.]] | ||
[[Category: FMD]] | [[Category: FMD]] | ||
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[[Category: serine/threonine protein kinase]] | [[Category: serine/threonine protein kinase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:47:52 2008'' |
Revision as of 12:47, 21 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
Page seeded by OCA on Thu Feb 21 14:47:52 2008
