4IWD

Structure of dually phosphorylated c-MET receptor kinase in complex with an MK-8033 analog

Summary for 4IWD

• Entry DOI: 10.2210/pdb4iwd/pdb
• Related: 3r7o
• Descriptor: Hepatocyte growth factor receptor, 1-{5-oxo-3-[1-(piperidin-4-yl)-1H-pyrazol-4-yl]-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl}-N-(pyridin-2-ylmethyl)methanesulfonamide (3 entities in total)
• Functional Keywords: protein kinase, tyrosine kinase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Membrane; Single-pass type I membrane protein. Isoform 3: Secreted: P08581
• Total number of polymer chains: 1
• Total formula weight: 35550.94

Authors

Soisson, S.M.,Northrup, A.,Rickert, K.,Patel, S.,Allison, T. (deposition date: 2013-01-23, release date: 2013-12-11, Last modification date: 2017-11-15)

• Primary citation: Northrup, A.B.,Katcher, M.H.,Altman, M.D.,Chenard, M.,Daniels, M.H.,Deshmukh, S.V.,Falcone, D.,Guerin, D.J.,Hatch, H.,Li, C.,Lu, W.,Lutterbach, B.,Allison, T.J.,Patel, S.B.,Reilly, J.F.,Reutershan, M.,Rickert, K.W.,Rosenstein, C.,Soisson, S.M.,Szewczak, A.A.,Walker, D.,Wilson, K.,Young, J.R.,Pan, B.S.,Dinsmore, C.J.; Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.; J.Med.Chem., 56:2294-2310, 2013; PubMed: 23379595; DOI: 10.1021/jm301619u

Experimental method

X-RAY DIFFRACTION (1.99 Å)