2pl0

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{{STRUCTURE_2pl0| PDB=2pl0 | SCENE= }}
{{STRUCTURE_2pl0| PDB=2pl0 | SCENE= }}
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'''LCK bound to imatinib'''
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===LCK bound to imatinib===
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==Overview==
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We report a clustering of public human protein kinase structures based on the conformations of two structural elements, the activation segment and the C-helix, revealing three discrete clusters. One cluster includes kinases in catalytically active conformations. Each of the other clusters contains a distinct inactive conformation. Typically, kinases adopt at most one of the inactive conformations in available X-ray structures, implying that one of the conformations is preferred for many kinases. The classification is consistent with selectivity profiles of several well-characterized kinase inhibitors. We show further that inhibitor selectivity profiles guide kinase classification. For example, selective inhibition of lck among src-family kinases by imatinib (Gleevec) suggests that the relative stabilities of inactive conformations of lck are different from other src-family kinases. We report the X-ray structure of the lck/imatinib complex, confirming that the conformation adopted by lck is distinct from other structurally-characterized src-family kinases and instead resembles kinases abl1 and kit in complex with imatinib. Our classification creates new paths for designing small-molecule inhibitors. Proteins 2008. (c) 2007 Wiley-Liss, Inc.
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{{ABSTRACT_PUBMED_17910071}}
==Disease==
==Disease==
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[[Category: Kinase phosphorylation]]
[[Category: Kinase phosphorylation]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 13:19:48 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 06:09:40 2008''

Revision as of 03:09, 28 July 2008

Image:2pl0.png

Template:STRUCTURE 2pl0

Contents

LCK bound to imatinib

Template:ABSTRACT PUBMED 17910071

Disease

Known disease associated with this structure: SCID due to LCK deficiency OMIM:[153390]

About this Structure

2PL0 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Classifying protein kinase structures guides use of ligand-selectivity profiles to predict inactive conformations: Structure of lck/imatinib complex., Jacobs MD, Caron PR, Hare BJ, Proteins. 2007 Oct 1;70(4):1451-1460. PMID:17910071

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