2pvf: Difference between revisions

Revision as of 13:52, 4 May 2008

Crystal Structure of Tyrosine Phosphorylated Activated FGF Receptor 2 (FGFR2) Kinase Domain in Complex with ATP Analog and Substrate Peptide

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

2PVF is a Protein complex structure of sequences from Homo sapiens. 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 Page seeded by OCA on Sun May 4 13:52:05 2008

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OCA

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 [[Image:2pvf.jpg|left|200px]]
- {{Structure
+<!--
-|PDB= 2pvf |SIZE=350|CAPTION= <scene name='initialview01'>2pvf</scene>, resolution 1.8&Aring;
+The line below this paragraph, containing "STRUCTURE_2pvf", creates the "Structure Box" on the page.
-|SITE=
+You may change the PDB parameter (which sets the PDB file loaded into the applet)
-|LIGAND= <scene name='pdbligand=ABG:ADENOSINE+5&#39;-[BETA,GAMMA-METHYLENE]TRIPHOSPHATE'>ABG</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</scene>
+or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-|ACTIVITY= <span class='plainlinks'>[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] </span>
+or leave the SCENE parameter empty for the default display.
-|GENE= FGFR2, BEK, KSAM ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
+-->
-|DOMAIN=
+{{STRUCTURE_2pvf|  PDB=2pvf  |  SCENE=  }}
-|RELATEDENTRY=[[2psq|2PSQ]], [[2pvy|2PVY]], [[2pwl|2PWL]], [[2py3|2PY3]], [[2pz5|2PZ5]], [[2pzp|2PZP]], [[2pzr|2PZR]], [[2q0b|2Q0B]]
-|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2pvf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2pvf OCA], [http://www.ebi.ac.uk/pdbsum/2pvf PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2pvf RCSB]</span>
-}}
 '''Crystal Structure of Tyrosine Phosphorylated Activated FGF Receptor 2 (FGFR2) Kinase Domain in Complex with ATP Analog and Substrate Peptide'''
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 [[Category: Chen, H.]]
 [[Category: Mohammadi, M.]]
-[[Category: kinase domain fold consisting of n- and c-lobe]]
+[[Category: Kinase domain fold consisting of n- and c-lobe]]
-[[Category: transferase]]
+[[Category: Transferase]]
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 13:52:05 2008''
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:41:18 2008''