1p2a

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{{STRUCTURE_1p2a| PDB=1p2a | SCENE= }}
{{STRUCTURE_1p2a| PDB=1p2a | SCENE= }}
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'''The structure of cyclin dependent kinase 2 (CKD2) with a trisubstituted naphthostyril inhibitor'''
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===The structure of cyclin dependent kinase 2 (CKD2) with a trisubstituted naphthostyril inhibitor===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 12852944 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12852944}}
==About this Structure==
==About this Structure==
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[[Category: Cyclin dependent kinase]]
[[Category: Cyclin dependent kinase]]
[[Category: Naphthostyril oxindole]]
[[Category: Naphthostyril oxindole]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 04:35:17 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 18:04:10 2008''

Revision as of 15:04, 27 July 2008

Image:1p2a.png

Template:STRUCTURE 1p2a

The structure of cyclin dependent kinase 2 (CKD2) with a trisubstituted naphthostyril inhibitor

Template:ABSTRACT PUBMED 12852944

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

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