2q0b: Difference between revisions
New page: left|200px<br /> <applet load="2q0b" size="450" color="white" frame="true" align="right" spinBox="true" caption="2q0b, resolution 2.9Å" /> '''Crystal Strucure of ... |
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[[Image:2q0b. | [[Image:2q0b.jpg|left|200px]]<br /><applet load="2q0b" size="350" color="white" frame="true" align="right" spinBox="true" | ||
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caption="2q0b, resolution 2.9Å" /> | caption="2q0b, resolution 2.9Å" /> | ||
'''Crystal Strucure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic E565A Mutation Responsible for Pfeiffer Syndrome'''<br /> | '''Crystal Strucure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic E565A Mutation Responsible for Pfeiffer Syndrome'''<br /> | ||
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==Overview== | ==Overview== | ||
Activating mutations in the tyrosine kinase domain of receptor tyrosine, kinases (RTKs) cause cancer and skeletal disorders. Comparison of the, crystal structures of unphosphorylated and phosphorylated wild-type FGFR2, kinase domains with those of seven unphosphorylated pathogenic mutants, reveals an autoinhibitory "molecular brake" mediated by a triad of, residues in the kinase hinge region of all FGFRs. Structural analysis, shows that many other RTKs, including PDGFRs, VEGFRs, KIT, CSF1R, FLT3, TEK, and TIE, are also subject to regulation by this brake. Pathogenic, mutations activate FGFRs and other RTKs by disengaging the brake either, directly or indirectly. | Activating mutations in the tyrosine kinase domain of receptor tyrosine, kinases (RTKs) cause cancer and skeletal disorders. Comparison of the, crystal structures of unphosphorylated and phosphorylated wild-type FGFR2, kinase domains with those of seven unphosphorylated pathogenic mutants, reveals an autoinhibitory "molecular brake" mediated by a triad of, residues in the kinase hinge region of all FGFRs. Structural analysis, shows that many other RTKs, including PDGFRs, VEGFRs, KIT, CSF1R, FLT3, TEK, and TIE, are also subject to regulation by this brake. Pathogenic, mutations activate FGFRs and other RTKs by disengaging the brake either, directly or indirectly. | ||
==About this Structure== | ==About this Structure== | ||
2Q0B is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SO4 and ABG as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1] Full crystallographic information is available from [http:// | 2Q0B is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=SO4:'>SO4</scene> and <scene name='pdbligand=ABG:'>ABG</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Q0B OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 13:28:44 2008'' | ||
Revision as of 14:28, 23 January 2008
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Crystal Strucure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Pathogenic E565A Mutation Responsible for Pfeiffer Syndrome
OverviewOverview
Activating mutations in the tyrosine kinase domain of receptor tyrosine, kinases (RTKs) cause cancer and skeletal disorders. Comparison of the, crystal structures of unphosphorylated and phosphorylated wild-type FGFR2, kinase domains with those of seven unphosphorylated pathogenic mutants, reveals an autoinhibitory "molecular brake" mediated by a triad of, residues in the kinase hinge region of all FGFRs. Structural analysis, shows that many other RTKs, including PDGFRs, VEGFRs, KIT, CSF1R, FLT3, TEK, and TIE, are also subject to regulation by this brake. Pathogenic, mutations activate FGFRs and other RTKs by disengaging the brake either, directly or indirectly.
About this StructureAbout this Structure
2Q0B is a Single protein structure of sequence from Homo sapiens with and as ligands. Active as Receptor protein-tyrosine kinase, with EC number 2.7.10.1 Full crystallographic information is available from OCA.
ReferenceReference
A molecular brake in the kinase hinge region regulates the activity of receptor tyrosine kinases., Chen H, Ma J, Li W, Eliseenkova AV, Xu C, Neubert TA, Miller WT, Mohammadi M, Mol Cell. 2007 Sep 7;27(5):717-30. PMID:17803937
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