3DKG

Structure of Mutant(Y1248L) MET receptor tyrosine kinase in complex with inhibitor SGX-523

Summary for 3DKG

• Entry DOI: 10.2210/pdb3dkg/pdb
• Related: 3DKC 3DKF
• Descriptor: Hepatocyte growth factor receptor, CHLORIDE ION, 6-{[6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulfanyl}quinoline, ... (4 entities in total)
• Functional Keywords: drug discovery, c-met kinase, fragment based, membrane, receptor, transmembrane, oncoprotein
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 1
• Total formula weight: 36095.19

Authors

Hendle, J. (deposition date: 2008-06-24, release date: 2009-07-07, Last modification date: 2024-02-21)

• Primary citation: 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.; SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo.; Mol.Cancer Ther., 8:3181-3190, 2009; PubMed: 19934279; DOI: 10.1158/1535-7163.MCT-09-0477

Experimental method

X-RAY DIFFRACTION (1.91 Å)