2obj

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[[Image:2obj.gif|left|200px]]
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{{Seed}}
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[[Image:2obj.png|left|200px]]
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{{STRUCTURE_2obj| PDB=2obj | SCENE= }}
{{STRUCTURE_2obj| PDB=2obj | SCENE= }}
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'''Crystal structure of human PIM-1 Kinase in complex with inhibitor'''
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===Crystal structure of human PIM-1 Kinase in complex with inhibitor===
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==Overview==
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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.
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The line below this paragraph, {{ABSTRACT_PUBMED_17251021}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 17251021 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17251021}}
==About this Structure==
==About this Structure==
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[[Category: Pyridone]]
[[Category: Pyridone]]
[[Category: Serine/threonine kinase]]
[[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 Jul 28 01:57:33 2008''

Revision as of 22:57, 27 July 2008

Image:2obj.png

Template:STRUCTURE 2obj

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

Template:ABSTRACT PUBMED 17251021

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 Mon Jul 28 01:57:33 2008

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