1fpu

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[[Image:1fpu.gif|left|200px]]
[[Image:1fpu.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1fpu |SIZE=350|CAPTION= <scene name='initialview01'>1fpu</scene>, resolution 2.4&Aring;
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The line below this paragraph, containing "STRUCTURE_1fpu", 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=PRC:N-[4-METHYL-3-[[4-(3-PYRIDINYL)-2-PYRIMIDINYL]AMINO]PHENYL]-3-PYRIDINECARBOXAMIDE'>PRC</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=
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-->
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|DOMAIN=
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{{STRUCTURE_1fpu| PDB=1fpu | 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=1fpu FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1fpu OCA], [http://www.ebi.ac.uk/pdbsum/1fpu PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1fpu RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF ABL KINASE DOMAIN IN COMPLEX WITH A SMALL MOLECULE INHIBITOR'''
'''CRYSTAL STRUCTURE OF ABL KINASE DOMAIN IN COMPLEX WITH A SMALL MOLECULE INHIBITOR'''
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[[Category: Pellicena, P.]]
[[Category: Pellicena, P.]]
[[Category: Schindler, T.]]
[[Category: Schindler, T.]]
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[[Category: activation loop]]
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[[Category: Activation loop]]
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[[Category: kinase]]
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[[Category: Kinase]]
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[[Category: kinase inhibitor]]
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[[Category: Kinase inhibitor]]
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[[Category: sti-571]]
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[[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 Sun Mar 30 20:27:55 2008''
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Revision as of 13:37, 2 May 2008

Image:1fpu.gif

Template:STRUCTURE 1fpu

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


Overview

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.

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 Page seeded by OCA on Fri May 2 16:37:22 2008

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