1p2a
From Proteopedia
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'''The structure of cyclin dependent kinase 2 (CKD2) with a trisubstituted naphthostyril inhibitor''' | '''The structure of cyclin dependent kinase 2 (CKD2) with a trisubstituted naphthostyril inhibitor''' | ||
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[[Category: Yang, H.]] | [[Category: Yang, H.]] | ||
[[Category: Yin, X.]] | [[Category: Yin, X.]] | ||
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| - | [[Category: | + | [[Category: Naphthostyril oxindole]] |
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Revision as of 01:35, 3 May 2008
The structure of cyclin dependent kinase 2 (CKD2) with a trisubstituted naphthostyril inhibitor
Overview
A novel class of 3,5,6-trisubstituted naphthostyril analogues was designed and synthesized to study the structure-activity relationship for inhibition of cyclin-dependent kinase 2 (CDK2). These compounds, particularly molecules with side-chain modifications providing additional hydrogen bonding capability, were demonstrated to be potent CDK2 inhibitors with cellular activities consistent with CDK2 inhibition. These molecules inhibited tumor cell proliferation and G1-S and G2-M cell-cycle progression in vitro. The X-ray crystal structure of a 2-aminoethyleneamine derivative bound to CDK2, refined to 2.5A resolution, is presented.
About this Structure
1P2A is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
3,5,6-Trisubstituted naphthostyrils as CDK2 inhibitors., Liu JJ, Dermatakis A, Lukacs C, Konzelmann F, Chen Y, Kammlott U, Depinto W, Yang H, Yin X, Chen Y, Schutt A, Simcox ME, Luk KC, Bioorg Med Chem Lett. 2003 Aug 4;13(15):2465-8. PMID:12852944 Page seeded by OCA on Sat May 3 04:35:17 2008
