1opl

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[[Image:1opl.jpg|left|200px]]
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[[Image:1opl.png|left|200px]]
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==Overview==
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{{ABSTRACT_12654251}}
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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.
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==About this Structure==
==About this Structure==
1OPL is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. The following page contains interesting information on the relation of 1OPL with [[http://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/pdb43_1.html Src Tyrosine Kinase]]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1OPL OCA].
1OPL is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. The following page contains interesting information on the relation of 1OPL with [[http://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/pdb43_1.html Src Tyrosine Kinase]]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1OPL OCA].
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==Reference==
 
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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:[http://www.ncbi.nlm.nih.gov/pubmed/12654251 12654251]
 
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: Young, M A.]]
[[Category: Young, M A.]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 04:08:04 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Jun 26 17:47:58 2008''

Revision as of 14:47, 26 June 2008


PDB ID 1opl

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1opl, resolution 3.42Å ()
Ligands: ,
Gene: Abl (Homo sapiens)
Activity: Transferase, with EC number and 2.7.10.2 2.7.10.1 and 2.7.10.2
Related: 1opj, 1opk
Resources: FirstGlance, OCA, RCSB, PDBsum
Coordinates: save as pdb, mmCIF, xml



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


Template:ABSTRACT 12654251

About this Structure

1OPL is a Single protein structure of sequence from Homo sapiens. The following page contains interesting information on the relation of 1OPL with [Src Tyrosine Kinase]. Full crystallographic information is available from OCA.

Page seeded by OCA on Thu Jun 26 17:47:58 2008

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