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TitleStructural basis for selective small molecule kinase inhibition of activated c-Met.
Journal, issue, pagesJ. Biol. Chem., Vol. 286, Page 11218-11225, Year 2011
Publish dateJan 3, 2011 (structure data deposition date)
AuthorsRickert, K.W. / Patel, S.B. / Allison, T.J. / Byrne, N.J. / Darke, P.L. / Ford, R.E. / Guerin, D.J. / Hall, D.L. / Kornienko, M. / Lu, J. ...Rickert, K.W. / Patel, S.B. / Allison, T.J. / Byrne, N.J. / Darke, P.L. / Ford, R.E. / Guerin, D.J. / Hall, D.L. / Kornienko, M. / Lu, J. / Munshi, S.K. / Reid, J.C. / Shipman, J.M. / Stanton, E.F. / Wilson, K.J. / Young, J.R. / Soisson, S.M. / Lumb, K.J.
External linksJ. Biol. Chem. / PubMed:21247903
MethodsX-ray diffraction
Resolution1.6 - 2.3 Å
Structure data

PDB-3q6u:
Structure of the apo MET receptor kinase in the dually-phosphorylated, activated state
Method: X-RAY DIFFRACTION / Resolution: 1.6 Å

PDB-3q6w:
Structure of dually-phosphorylated MET receptor kinase in complex with an MK-2461 analog with specificity for the activated receptor
Method: X-RAY DIFFRACTION / Resolution: 1.75 Å

PDB-3r7o:
Structure of dually phosphorylated c-MET receptor kinase in complex with an MK-2461 analog
Method: X-RAY DIFFRACTION / Resolution: 2.3 Å

Chemicals

ChemComp-HOH:
WATER

ChemComp-Q6W:
3-{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)propanamide

ChemComp-M61:
N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N'-{5-oxo-3-[1-(piperidin-4-yl)-1H-pyrazol-4-yl]-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl}sulfuric diamide

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / tyrosine kinase / transferase/transferase inhibitor / two phosphotyrosine resiudes / transferase-transferase inhibitor complex / phosphotyrosine / 1234 / 1235

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