2hiw

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[[Image:2hiw.gif|left|200px]]
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{{STRUCTURE_2hiw| PDB=2hiw | SCENE= }}
{{STRUCTURE_2hiw| PDB=2hiw | SCENE= }}
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'''Crystal Structure of Inactive Conformation Abl Kinase Catalytic Domain Complexed with Type II Inhibitor'''
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===Crystal Structure of Inactive Conformation Abl Kinase Catalytic Domain Complexed with Type II Inhibitor===
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==Overview==
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Kinase inhibitors that bind to the ATP cleft can be broadly classified into two groups: those that bind exclusively to the ATP site with the kinase assuming a conformation otherwise conducive to phosphotransfer (type I), and those that exploit a hydrophobic site immediately adjacent to the ATP pocket made accessible by a conformational rearrangement of the activation loop (type II). To date, all type II inhibitors were discovered by using structure-activity-guided optimization strategies. Here, we describe a general pharmacophore model of type II inhibition that enables a rational "hybrid-design" approach whereby a 3-trifluoromethylbenzamide functionality is appended to four distinct type I scaffolds in order to convert them into their corresponding type II counterparts. We demonstrate that the designed compounds function as type II inhibitors by using biochemical and cellular kinase assays and by cocrystallography with Abl.
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(as it appears on PubMed at http://www.pubmed.gov), where 16873026 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16873026}}
==About this Structure==
==About this Structure==
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[[Category: Lee, C.]]
[[Category: Lee, C.]]
[[Category: Kinase domain]]
[[Category: Kinase domain]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 06:21:00 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 13:33:22 2008''

Revision as of 10:33, 29 July 2008

Image:2hiw.png

Template:STRUCTURE 2hiw

Crystal Structure of Inactive Conformation Abl Kinase Catalytic Domain Complexed with Type II Inhibitor

Template:ABSTRACT PUBMED 16873026

About this Structure

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

Reference

A general strategy for creating "inactive-conformation" abl inhibitors., Okram B, Nagle A, Adrian FJ, Lee C, Ren P, Wang X, Sim T, Xie Y, Wang X, Xia G, Spraggon G, Warmuth M, Liu Y, Gray NS, Chem Biol. 2006 Jul;13(7):779-86. PMID:16873026

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