1p2a
From Proteopedia
(New page: 200px<br /> <applet load="1p2a" size="450" color="white" frame="true" align="right" spinBox="true" caption="1p2a, resolution 2.5Å" /> '''The structure of cyc...) |
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| - | [[Image:1p2a. | + | [[Image:1p2a.jpg|left|200px]]<br /><applet load="1p2a" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="1p2a, resolution 2.5Å" /> | caption="1p2a, resolution 2.5Å" /> | ||
'''The structure of cyclin dependent kinase 2 (CKD2) with a trisubstituted naphthostyril inhibitor'''<br /> | '''The structure of cyclin dependent kinase 2 (CKD2) with a trisubstituted naphthostyril inhibitor'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1P2A 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 5BN as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 1P2A 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=5BN:'>5BN</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1P2A OCA]. |
==Reference== | ==Reference== | ||
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[[Category: naphthostyril oxindole]] | [[Category: naphthostyril oxindole]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:38:21 2008'' |
Revision as of 14:38, 15 February 2008
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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 with as ligand. 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
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