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| {{STRUCTURE_2pl0| PDB=2pl0 | SCENE= }} | | {{STRUCTURE_2pl0| PDB=2pl0 | SCENE= }} |
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| '''LCK bound to imatinib'''
| | ===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.
| | The line below this paragraph, {{ABSTRACT_PUBMED_17910071}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 17910071 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_17910071}} |
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| ==Disease== | | ==Disease== |
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| [[Category: Kinase phosphorylation]] | | [[Category: Kinase phosphorylation]] |
| [[Category: Transferase]] | | [[Category: Transferase]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 13:19:48 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 06:09:40 2008'' |
