2pl0

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[[Image:2pl0.jpg|left|200px]]
[[Image:2pl0.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2pl0 |SIZE=350|CAPTION= <scene name='initialview01'>2pl0</scene>, resolution 2.800&Aring;
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The line below this paragraph, containing "STRUCTURE_2pl0", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Sti+Binding+Site+For+Residue+A+200'>AC1</scene>
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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=STI:4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE'>STI</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_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= LCK ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2pl0| PDB=2pl0 | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2pl0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2pl0 OCA], [http://www.ebi.ac.uk/pdbsum/2pl0 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2pl0 RCSB]</span>
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}}
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'''LCK bound to imatinib'''
'''LCK bound to imatinib'''
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Jacobs, M D.]]
[[Category: Jacobs, M D.]]
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[[Category: kinase phosphorylation]]
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[[Category: Kinase phosphorylation]]
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[[Category: transferase]]
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[[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 Mar 31 04:37:21 2008''
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Revision as of 10:19, 4 May 2008

Image:2pl0.jpg

Template:STRUCTURE 2pl0

LCK bound to imatinib


Contents

Overview

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.

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 Page seeded by OCA on Sun May 4 13:19:48 2008

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OCA

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