1fpu

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[[Image:1fpu.gif|left|200px]]
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{{STRUCTURE_1fpu| PDB=1fpu | SCENE= }}
{{STRUCTURE_1fpu| PDB=1fpu | SCENE= }}
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'''CRYSTAL STRUCTURE OF ABL KINASE DOMAIN IN COMPLEX WITH A SMALL MOLECULE INHIBITOR'''
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===CRYSTAL STRUCTURE OF ABL KINASE DOMAIN IN COMPLEX WITH A SMALL MOLECULE INHIBITOR===
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==Overview==
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The inadvertent activation of the Abelson tyrosine kinase (Abl) causes chronic myelogenous leukemia (CML). A small-molecule inhibitor of Abl (STI-571) is effective in the treatment of CML. We report the crystal structure of the catalytic domain of Abl, complexed to a variant of STI-571. Critical to the binding of STI-571 is the adoption by the kinase of an inactive conformation, in which a centrally located "activation loop" is not phosphorylated. The conformation of this loop is distinct from that in active protein kinases, as well as in the inactive form of the closely related Src kinases. These results suggest that compounds that exploit the distinctive inactivation mechanisms of individual protein kinases can achieve both high affinity and high specificity.
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(as it appears on PubMed at http://www.pubmed.gov), where 10988075 is the PubMed ID number.
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{{ABSTRACT_PUBMED_10988075}}
==About this Structure==
==About this Structure==
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[[Category: Kinase inhibitor]]
[[Category: Kinase inhibitor]]
[[Category: Sti-571]]
[[Category: Sti-571]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 16:37:22 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 03:45:15 2008''

Revision as of 00:45, 1 July 2008

Image:1fpu.png

Template:STRUCTURE 1fpu

CRYSTAL STRUCTURE OF ABL KINASE DOMAIN IN COMPLEX WITH A SMALL MOLECULE INHIBITOR

Template:ABSTRACT PUBMED 10988075

About this Structure

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

Reference

Structural mechanism for STI-571 inhibition of abelson tyrosine kinase., Schindler T, Bornmann W, Pellicena P, Miller WT, Clarkson B, Kuriyan J, Science. 2000 Sep 15;289(5486):1938-42. PMID:10988075

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