1h07

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[[Image:1h07.gif|left|200px]]
[[Image:1h07.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1h07 |SIZE=350|CAPTION= <scene name='initialview01'>1h07</scene>, resolution 1.85&Aring;
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The line below this paragraph, containing "STRUCTURE_1h07", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=MFP:Mfq+Binding+Site+For+Chain+A'>MFP</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=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=MFP:((2-BROMO-4-METHYLPHENYL){6-[(4-{[(2R)-3-(DIMETHYLAMINO)-2-HYDROXYPROPYL]OXY}PHENYL)AMINO]PYRIMIDIN-4-YL}AMINO)ACETONITRILE'>MFP</scene>, <scene name='pdbligand=MFQ:((2-BROMO-4-METHYLPHENYL){6-[(4-{[(2S)-3-(DIMETHYLAMINO)-2-HYDROXYPROPYL]OXY}PHENYL)AMINO]PYRIMIDIN-4-YL}AMINO)ACETONITRILE'>MFQ</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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-->
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|DOMAIN=
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{{STRUCTURE_1h07| PDB=1h07 | 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=1h07 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1h07 OCA], [http://www.ebi.ac.uk/pdbsum/1h07 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1h07 RCSB]</span>
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}}
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'''CDK2 IN COMPLEX WITH A DISUBSTITUTED 4, 6-BIS ANILINO PYRIMIDINE CDK4 INHIBITOR'''
'''CDK2 IN COMPLEX WITH A DISUBSTITUTED 4, 6-BIS ANILINO PYRIMIDINE CDK4 INHIBITOR'''
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[[Category: Pease, J E.]]
[[Category: Pease, J E.]]
[[Category: Tucker, J A.]]
[[Category: Tucker, J A.]]
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[[Category: serine/threonine-protein kinase,mitosis,transferase]]
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[[Category: Serine/threonine-protein kinase,mitosis,transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 18:14:57 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 20:54:59 2008''
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Revision as of 15:14, 2 May 2008

Image:1h07.gif

Template:STRUCTURE 1h07

CDK2 IN COMPLEX WITH A DISUBSTITUTED 4, 6-BIS ANILINO PYRIMIDINE CDK4 INHIBITOR


Overview

Using a high-throughput screening campaign, we identified the 4,6-bis anilino pyrimidines as inhibitors of the cyclin-dependent kinase, CDK4. Herein we describe the further chemical modification and use of X-ray crystallography to develop potent and selective in vitro inhibitors of CDK4.

About this Structure

1H07 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines., Beattie JF, Breault GA, Ellston RP, Green S, Jewsbury PJ, Midgley CJ, Naven RT, Minshull CA, Pauptit RA, Tucker JA, Pease JE, Bioorg Med Chem Lett. 2003 Sep 15;13(18):2955-60. PMID:12941311 Page seeded by OCA on Fri May 2 18:14:57 2008

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OCA

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