1opk

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[[Image:1opk.gif|left|200px]]
[[Image:1opk.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1opk |SIZE=350|CAPTION= <scene name='initialview01'>1opk</scene>, resolution 1.80&Aring;
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The line below this paragraph, containing "STRUCTURE_1opk", creates the "Structure Box" on the page.
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|SITE=
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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=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=MYR:MYRISTIC+ACID'>MYR</scene>, <scene name='pdbligand=P16:6-(2,6-DICHLOROPHENYL)-2-{[3-(HYDROXYMETHYL)PHENYL]AMINO}-8-METHYLPYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONE'>P16</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/Transferase Transferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 and 2.7.10.2 2.7.10.1 and 2.7.10.2] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= ABL1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 Mus musculus])
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-->
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|DOMAIN=
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{{STRUCTURE_1opk| PDB=1opk | SCENE= }}
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|RELATEDENTRY=[[1opj|1OPJ]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1opk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1opk OCA], [http://www.ebi.ac.uk/pdbsum/1opk PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1opk RCSB]</span>
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}}
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'''Structural basis for the auto-inhibition of c-Abl tyrosine kinase'''
'''Structural basis for the auto-inhibition of c-Abl tyrosine kinase'''
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[[Category: Veach, D.]]
[[Category: Veach, D.]]
[[Category: Young, M A.]]
[[Category: Young, M A.]]
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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 Sat May 3 04:07:50 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:48:33 2008''
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Revision as of 01:07, 3 May 2008

Image:1opk.gif

Template:STRUCTURE 1opk

Structural basis for the auto-inhibition of c-Abl tyrosine kinase


Overview

c-Abl is normally regulated by an autoinhibitory mechanism, the disruption of which leads to chronic myelogenous leukemia. The details of this mechanism have been elusive because c-Abl lacks a phosphotyrosine residue that triggers the assembly of the autoinhibited form of the closely related Src kinases by internally engaging the SH2 domain. Crystal structures of c-Abl show that the N-terminal myristoyl modification of c-Abl 1b binds to the kinase domain and induces conformational changes that allow the SH2 and SH3 domains to dock onto it. Autoinhibited c-Abl forms an assembly that is strikingly similar to that of inactive Src kinases but with specific differences that explain the differential ability of the drug STI-571/Gleevec/imatinib (STI-571) to inhibit the catalytic activity of Abl, but not that of c-Src.

About this Structure

1OPK is a Single protein structure of sequence from Mus musculus. Full crystallographic information is available from OCA.

Reference

Structural basis for the autoinhibition of c-Abl tyrosine kinase., Nagar B, Hantschel O, Young MA, Scheffzek K, Veach D, Bornmann W, Clarkson B, Superti-Furga G, Kuriyan J, Cell. 2003 Mar 21;112(6):859-71. PMID:12654251 Page seeded by OCA on Sat May 3 04:07:50 2008

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OCA

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