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2a0c

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{{STRUCTURE_2a0c| PDB=2a0c | SCENE= }}
{{STRUCTURE_2a0c| PDB=2a0c | SCENE= }}
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'''Human CDK2 in complex with olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor'''
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===Human CDK2 in complex with olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor===
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==Overview==
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The study describes the protein kinase selectivity profile, as well as the binding mode of olomoucine II in the catalytic cleft of CDK2, as determined from cocrystal analysis. Apart from the main cell cycle-regulating kinase CDK2, olomoucine II exerts specificity for CDK7 and CDK9, with important functions in the regulation of RNA transcription. In vitro anticancer activity of the inhibitor in a panel of tumor cell lines shows a wide potency range with a slight preference for cells harboring a wild-type p53 gene. Cell-based assays confirmed activation of p53 protein levels and events leading to accumulation of p21(WAF1). Additionally, in olomoucine II-treated cells, Mdm2 was found to form a complex with the ribosomal protein L11, which inhibits Mdm2 ubiquitin ligase function. We conclude that perturbations in RNA synthesis may lead to activation of p53 and that this contributes to the antiproliferative potency of cyclindependent kinase inhibitors.
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The line below this paragraph, {{ABSTRACT_PUBMED_16003486}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16003486 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16003486}}
==About this Structure==
==About this Structure==
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[[Category: Serine/threonine-protein kinase]]
[[Category: Serine/threonine-protein kinase]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 18:27:05 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 04:21:18 2008''

Revision as of 01:21, 29 July 2008

Image:2a0c.png

Template:STRUCTURE 2a0c

Human CDK2 in complex with olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor

Template:ABSTRACT PUBMED 16003486

About this Structure

2A0C is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Antiproliferative activity of olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor., Krystof V, McNae IW, Walkinshaw MD, Fischer PM, Muller P, Vojtesek B, Orsag M, Havlicek L, Strnad M, Cell Mol Life Sci. 2005 Aug;62(15):1763-71. PMID:16003486

Page seeded by OCA on Tue Jul 29 04:21:18 2008

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