2c6t

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[[Image:2c6t.gif|left|200px]]
[[Image:2c6t.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2c6t |SIZE=350|CAPTION= <scene name='initialview01'>2c6t</scene>, resolution 2.61&Aring;
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The line below this paragraph, containing "STRUCTURE_2c6t", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Dt5+Binding+Site+For+Chain+C'>AC1</scene>
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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=DT5:4-{[5-(CYCLOHEXYLOXY)[1,2,4]TRIAZOLO[1,5-A]PYRIMIDIN-7-YL]AMINO}BENZENESULFONAMIDE'>DT5</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</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=
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|DOMAIN=
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{{STRUCTURE_2c6t| PDB=2c6t | 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=2c6t FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2c6t OCA], [http://www.ebi.ac.uk/pdbsum/2c6t PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2c6t RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF THE HUMAN CDK2 COMPLEXED WITH THE TRIAZOLOPYRIMIDINE INHIBITOR'''
'''CRYSTAL STRUCTURE OF THE HUMAN CDK2 COMPLEXED WITH THE TRIAZOLOPYRIMIDINE INHIBITOR'''
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[[Category: Richardson, C M.]]
[[Category: Richardson, C M.]]
[[Category: Surgenor, A E.]]
[[Category: Surgenor, A E.]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: cdk2]]
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[[Category: Cdk2]]
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[[Category: cell cycle]]
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[[Category: Cell cycle]]
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[[Category: complex (transferase/cyclin2)]]
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[[Category: Mitosis]]
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[[Category: mitosis]]
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[[Category: Phosphorylation]]
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[[Category: phosphorylation]]
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[[Category: Serine/threonine protein kinase]]
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[[Category: serine/threonine protein kinase]]
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[[Category: Triazolopyrimidine inhibitor]]
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[[Category: triazolopyrimidine inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 21:21:01 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:17:12 2008''
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Revision as of 18:21, 3 May 2008

Image:2c6t.gif

Template:STRUCTURE 2c6t

CRYSTAL STRUCTURE OF THE HUMAN CDK2 COMPLEXED WITH THE TRIAZOLOPYRIMIDINE INHIBITOR


Overview

Crystallographic and modelling data, in conjunction with a medicinal chemistry template-hopping approach, led to the identification of a series of novel and potent inhibitors of human cyclin-dependent kinase 2 (CDK2), with selectivity over glycogen synthase kinase-3beta (GSK-3beta). One example had a CDK2 IC(50) of 120 nM and showed selectivity over GSK-3beta of 167-fold.

About this Structure

2C6T is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR., Richardson CM, Williamson DS, Parratt MJ, Borgognoni J, Cansfield AD, Dokurno P, Francis GL, Howes R, Moore JD, Murray JB, Robertson A, Surgenor AE, Torrance CJ, Bioorg Med Chem Lett. 2006 Mar 1;16(5):1353-7. Epub 2005 Dec 1. PMID:16325401 Page seeded by OCA on Sat May 3 21:21:01 2008

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OCA

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