1agw

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[[Image:1agw.gif|left|200px]]
[[Image:1agw.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1agw |SIZE=350|CAPTION= <scene name='initialview01'>1agw</scene>, resolution 2.4&Aring;
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The line below this paragraph, containing "STRUCTURE_1agw", 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=SU2:3-[4-(1-FORMYLPIPERAZIN-4-YL)-BENZYLIDENYL]-2-INDOLINONE'>SU2</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_1agw| PDB=1agw | 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=1agw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1agw OCA], [http://www.ebi.ac.uk/pdbsum/1agw PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1agw RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH SU4984 INHIBITOR'''
'''CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH SU4984 INHIBITOR'''
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[[Category: Mohammadi, M.]]
[[Category: Mohammadi, M.]]
[[Category: Schlessinger, J.]]
[[Category: Schlessinger, J.]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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[[Category: phosphorylation]]
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[[Category: Phosphorylation]]
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[[Category: protein kinase]]
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[[Category: Protein kinase]]
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[[Category: transferase]]
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[[Category: Transferase]]
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[[Category: tyrosine-protein kinase]]
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[[Category: Tyrosine-protein kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 10:15:09 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 18:40:01 2008''
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Revision as of 07:15, 2 May 2008

Image:1agw.gif

Template:STRUCTURE 1agw

CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH SU4984 INHIBITOR


Overview

A new class of protein tyrosine kinase inhibitors was identified that is based on an oxindole core (indolinones). Two compounds from this class inhibited the kinase activity of fibroblast growth factor receptor 1 (FGFR1) and showed differential specificity toward other receptor tyrosine kinases. Crystal structures of the tyrosine kinase domain of FGFR1 in complex with the two compounds were determined. The oxindole occupies the site in which the adenine of adenosine triphosphate binds, whereas the moieties that extend from the oxindole contact residues in the hinge region between the two kinase lobes. The more specific inhibitor of FGFR1 induces a conformational change in the nucleotide-binding loop. This structural information will facilitate the design of new inhibitors for use in the treatment of cancer and other diseases in which cell signaling by tyrosine kinases plays a crucial role in disease pathogenesis.

About this Structure

1AGW is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors., Mohammadi M, McMahon G, Sun L, Tang C, Hirth P, Yeh BK, Hubbard SR, Schlessinger J, Science. 1997 May 9;276(5314):955-60. PMID:9139660 Page seeded by OCA on Fri May 2 10:15:09 2008

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