|Entry||Database: PDB / ID: 3dkf|
|Title||Structure of MET receptor tyrosine kinase in complex with inhibitor SGX-523|
|Components||Hepatocyte growth factor receptorC-Met|
|Keywords||ONCOPROTEIN / DRUG DISCOVERY / c-MET KINASE / FRAGMENT BASED / Membrane / Receptor / Transmembrane|
|Function / homology|
Function and homology information
hepatocyte growth factor receptor activity / Drug-mediated inhibition of MET activation / MET activates STAT3 / endothelial cell morphogenesis / negative regulation of hydrogen peroxide-mediated programmed cell death / negative regulation of guanyl-nucleotide exchange factor activity / MET interacts with TNS proteins / MET Receptor Activation / positive regulation of endothelial cell chemotaxis / semaphorin receptor activity ...hepatocyte growth factor receptor activity / Drug-mediated inhibition of MET activation / MET activates STAT3 / endothelial cell morphogenesis / negative regulation of hydrogen peroxide-mediated programmed cell death / negative regulation of guanyl-nucleotide exchange factor activity / MET interacts with TNS proteins / MET Receptor Activation / positive regulation of endothelial cell chemotaxis / semaphorin receptor activity / MET receptor recycling / Sema4D mediated inhibition of cell attachment and migration / MET activates PTPN11 / pancreas development / negative regulation of Rho protein signal transduction / MET activates PI3K/AKT signaling / MET activates RAP1 and RAC1 / negative regulation of stress fiber assembly / negative regulation of thrombin-activated receptor signaling pathway / semaphorin-plexin signaling pathway / MET activates PTK2 signaling / branching morphogenesis of an epithelial tube / positive chemotaxis / establishment of skin barrier / MECP2 regulates neuronal receptors and channels / positive regulation of microtubule polymerization / MET activates RAS signaling / phagocytosis / negative regulation of autophagy / basal plasma membrane / InlB-mediated entry of Listeria monocytogenes into host cell / liver development / Negative regulation of MET activity / neuron differentiation / receptor protein-tyrosine kinase / transmembrane receptor protein tyrosine kinase activity / positive regulation of kinase activity / Constitutive Signaling by Aberrant PI3K in Cancer / PIP3 activates AKT signaling / nervous system development / transmembrane receptor protein tyrosine kinase signaling pathway / cell migration / PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling / RAF/MAP kinase cascade / protein tyrosine kinase activity / positive regulation of protein kinase B signaling / protein phosphatase binding / cell surface receptor signaling pathway / receptor complex / cell surface / signal transduction / plasma membrane => GO:0005886 / positive regulation of transcription by RNA polymerase II / extracellular region / membrane => GO:0016020 / ATP binding / identical protein binding / plasma membrane
Similarity search - Function
Tyrosine-protein kinase, HGF/MSP receptor / Plexin family / Plexin repeat / Plexin repeat / Sema domain / semaphorin domain / Sema domain superfamily / Sema domain profile. / Sema domain / IPT/TIG domain ...Tyrosine-protein kinase, HGF/MSP receptor / Plexin family / Plexin repeat / Plexin repeat / Sema domain / semaphorin domain / Sema domain superfamily / Sema domain profile. / Sema domain / IPT/TIG domain / ig-like, plexins, transcription factors / PSI domain / domain found in Plexins, Semaphorins and Integrins / IPT domain / Immunoglobulin E-set / Tyrosine kinase, catalytic domain / Tyrosine-protein kinase, catalytic domain / Tyrosine protein kinases specific active-site signature. / Tyrosine-protein kinase, active site / Protein tyrosine and serine/threonine kinase / Serine-threonine/tyrosine-protein kinase, catalytic domain / WD40/YVTN repeat-like-containing domain superfamily / Transferase(Phosphotransferase) domain 1 / Transferase(Phosphotransferase); domain 1 / Phosphorylase Kinase; domain 1 / Phosphorylase Kinase; domain 1 / Protein kinases ATP-binding region signature. / Protein kinase, ATP binding site / Immunoglobulin-like fold / Protein kinase domain profile. / Protein kinase domain / Protein kinase-like domain superfamily / 2-Layer Sandwich / Orthogonal Bundle / Mainly Alpha / Alpha Beta
Similarity search - Domain/homology
Chem-SX8 / Hepatocyte growth factor receptor
Similarity search - Component
|Biological species||Homo sapiens (human)|
|Method||X-RAY DIFFRACTION / SYNCHROTRON / Resolution: 1.8 Å|
|Citation||Journal: Mol.Cancer Ther. / Year: 2009|
Title: SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo.
Authors: Buchanan, S.G. / Hendle, J. / Lee, P.S. / Smith, C.R. / Bounaud, P.Y. / Jessen, K.A. / Tang, C.M. / Huser, N.H. / Felce, J.D. / Froning, K.J. / Peterman, M.C. / Aubol, B.E. / Gessert, S.F. / ...Authors: Buchanan, S.G. / Hendle, J. / Lee, P.S. / Smith, C.R. / Bounaud, P.Y. / Jessen, K.A. / Tang, C.M. / Huser, N.H. / Felce, J.D. / Froning, K.J. / Peterman, M.C. / Aubol, B.E. / Gessert, S.F. / Sauder, J.M. / Schwinn, K.D. / Russell, M. / Rooney, I.A. / Adams, J. / Leon, B.C. / Do, T.H. / Blaney, J.M. / Sprengeler, P.A. / Thompson, D.A. / Smyth, L. / Pelletier, L.A. / Atwell, S. / Holme, K. / Wasserman, S.R. / Emtage, S. / Burley, S.K. / Reich, S.H.
|Structure viewer||Molecule: |
Downloads & links
A: Hepatocyte growth factor receptor
|#1: Protein|| |
Mass: 35750.348 Da / Num. of mol.: 1 / Mutation: Y1194F, Y1234F, Y1235D
Source method: isolated from a genetically manipulated source
Source: (gene. exp.) Homo sapiens (human) / Gene: MET, hCG_38705, tcag7.66 / Cell line (production host): SF9 / Production host: Spodoptera frugiperda (fall armyworm) / References: UniProt: P08581
|#2: Chemical|| ChemComp-CL / |
|#3: Chemical|| ChemComp-SX8 / |
|#4: Water|| ChemComp-HOH / |
|Experiment||Method: X-RAY DIFFRACTION / Number of used crystals: 1|
|Crystal||Density Matthews: 2.23 Å3/Da / Density % sol: 44.82 %|
|Crystal grow||Temperature: 292 K / Method: vapor diffusion / pH: 7.5 |
Details: 20% ISOPROPANOL, 200 mM AMMONIUM ACETATE, 100 mM TRIS, pH 7.5, VAPOR DIFFUSION, temperature 292K
|Diffraction||Mean temperature: 100 K|
|Diffraction source||Source: SYNCHROTRON / Site: APS / Beamline: 31-ID / Wavelength: 0.97969 Å|
|Detector||Type: MAR CCD 165 mm / Detector: CCD / Date: Jan 19, 2007|
|Radiation||Monochromator: DIAMOND / Protocol: SINGLE WAVELENGTH / Monochromatic (M) / Laue (L): M / Scattering type: x-ray|
|Radiation wavelength||Wavelength: 0.97969 Å / Relative weight: 1|
|Reflection||Resolution: 1.8→34.986 Å / Num. obs: 24264 / % possible obs: 79.7 % / Redundancy: 4.3 % / Rmerge(I) obs: 0.055 / Net I/σ(I): 11.3|
|Refinement||Resolution: 1.8→34.986 Å / Occupancy max: 1 / Occupancy min: 0.35 / |
|Displacement parameters||Biso max: 70.78 Å2 / Biso mean: 28.781 Å2 / Biso min: 5.17 Å2|
|Refinement step||Cycle: LAST / Resolution: 1.8→34.986 Å|
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