1opk

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[[Image:1opk.gif|left|200px]]
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{{STRUCTURE_1opk| PDB=1opk | SCENE= }}
{{STRUCTURE_1opk| PDB=1opk | SCENE= }}
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'''Structural basis for the auto-inhibition of c-Abl tyrosine kinase'''
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===Structural basis for the auto-inhibition of c-Abl tyrosine kinase===
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==Overview==
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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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(as it appears on PubMed at http://www.pubmed.gov), where 12654251 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12654251}}
==About this Structure==
==About this Structure==
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[[Category: Young, M A.]]
[[Category: Young, M A.]]
[[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 Tue Jul 29 05:43:48 2008''

Revision as of 02:43, 29 July 2008

Image:1opk.png

Template:STRUCTURE 1opk

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

Template:ABSTRACT PUBMED 12654251

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 Tue Jul 29 05:43:48 2008

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