2obj

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[[Image:2obj.gif|left|200px]]
[[Image:2obj.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2obj |SIZE=350|CAPTION= <scene name='initialview01'>2obj</scene>, resolution 2.5&Aring;
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The line below this paragraph, containing "STRUCTURE_2obj", 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=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=VRV:6-(5-BROMO-2-HYDROXYPHENYL)-2-OXO-4-PHENYL-1,2-DIHYDROPYRIDINE-3-CARBONITRILE'>VRV</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_2obj| PDB=2obj | SCENE= }}
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|RELATEDENTRY=[[1xqz|1XQZ]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2obj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2obj OCA], [http://www.ebi.ac.uk/pdbsum/2obj PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2obj RCSB]</span>
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}}
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'''Crystal structure of human PIM-1 Kinase in complex with inhibitor'''
'''Crystal structure of human PIM-1 Kinase in complex with inhibitor'''
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[[Category: Yan, S.]]
[[Category: Yan, S.]]
[[Category: Yao, N.]]
[[Category: Yao, N.]]
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[[Category: human pim-1 kinase]]
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[[Category: Human pim-1 kinase]]
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[[Category: kinase inhibitor]]
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[[Category: Kinase inhibitor]]
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[[Category: kinase inhibitor complex]]
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[[Category: Kinase inhibitor complex]]
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[[Category: pim]]
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[[Category: Pim]]
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[[Category: pim-1]]
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[[Category: Pim-1]]
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[[Category: pim1]]
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[[Category: Pim1]]
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[[Category: pyridone]]
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[[Category: Pyridone]]
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[[Category: serine/threonine kinase]]
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[[Category: Serine/threonine kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 10:33:32 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:15:24 2008''
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Revision as of 07:33, 4 May 2008

Image:2obj.gif

Template:STRUCTURE 2obj

Crystal structure of human PIM-1 Kinase in complex with inhibitor


Overview

A novel series of highly potent substituted pyridone Pim-1 kinase inhibitors is described. Structural requirements for in vitro activity are outlined as well as a complex crystal structure with the most potent Pim-1 inhibitor reported (IC(50)=50 nM). A hydrogen bond matrix involving the Pim-1 inhibitor, two water molecules, and the catalytic core, together with a potential weak hydrogen bond between an aromatic hydrogen on the R(1) phenyl ring and a main-chain carbonyl of Pim-1, accounts for the overall potency of this inhibitor.

About this Structure

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

Reference

Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase., Cheney IW, Yan S, Appleby T, Walker H, Vo T, Yao N, Hamatake R, Hong Z, Wu JZ, Bioorg Med Chem Lett. 2007 Mar 15;17(6):1679-83. Epub 2007 Jan 4. PMID:17251021 Page seeded by OCA on Sun May 4 10:33:32 2008

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OCA

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