1fgi
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(New page: 200px<br /> <applet load="1fgi" size="450" color="white" frame="true" align="right" spinBox="true" caption="1fgi, resolution 2.5Å" /> '''CRYSTAL STRUCTURE OF...)
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Revision as of 14:46, 12 November 2007
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CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH SU5402 INHIBITOR
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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.
Disease
Known diseases associated with this structure: Atopic dermatitis, susceptibility to OMIM:[135940], Ichthyosis vulgaris OMIM:[135940], Jackson-Weiss syndrome OMIM:[136350], Kallmann syndrome 2 OMIM:[136350], Pfeiffer syndrome OMIM:[136350]
About this Structure
1FGI is a Single protein structure of sequence from Homo sapiens with SU1 as ligand. Active as Transferase, with EC number and 2.7.10.2 2.7.10.1 and 2.7.10.2 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
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