2a0c

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[[Image:2a0c.gif|left|200px]]
[[Image:2a0c.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2a0c |SIZE=350|CAPTION= <scene name='initialview01'>2a0c</scene>, resolution 1.95&Aring;
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The line below this paragraph, containing "STRUCTURE_2a0c", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=CK9:2-{[(2-{[(1R)-1-(HYDROXYMETHYL)PROPYL]AMINO}-9-ISOPROPYL-9H-PURIN-6-YL)AMINO]METHYL}PHENOL'>CK9</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= CDK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2a0c| PDB=2a0c | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2a0c FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2a0c OCA], [http://www.ebi.ac.uk/pdbsum/2a0c PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2a0c RCSB]</span>
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}}
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'''Human CDK2 in complex with olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor'''
'''Human CDK2 in complex with olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor'''
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[[Category: Walkinshaw, M D.]]
[[Category: Walkinshaw, M D.]]
[[Category: 3d-structure]]
[[Category: 3d-structure]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: cell cycle]]
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[[Category: Cell cycle]]
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[[Category: cell division,mitosis]]
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[[Category: Cell division,mitosis]]
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[[Category: inhibition]]
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[[Category: Inhibition]]
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[[Category: phosphorylation]]
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[[Category: Phosphorylation]]
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[[Category: protein kinase]]
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[[Category: Protein kinase]]
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[[Category: serine/threonine-protein kinase]]
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[[Category: Serine/threonine-protein kinase]]
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[[Category: transferase]]
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[[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 Mon Mar 31 01:46:14 2008''
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Revision as of 15:27, 3 May 2008

Image:2a0c.gif

Template:STRUCTURE 2a0c

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


Overview

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.

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 Sat May 3 18:27:05 2008

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