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Structure paper

TitleKIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients.
Journal, issue, pagesProc. Natl. Acad. Sci. USA, Vol. 106, Page 1542-1547, Year 2009
Publish dateJan 27, 2009 (structure data deposition date)
AuthorsGajiwala, K.S. / Wu, J.C. / Christensen, J. / Deshmukh, G.D. / Diehl, W. / DiNitto, J.P. / English, J.M. / Greig, M.J. / He, Y.A. / Jacques, S.L. ...Gajiwala, K.S. / Wu, J.C. / Christensen, J. / Deshmukh, G.D. / Diehl, W. / DiNitto, J.P. / English, J.M. / Greig, M.J. / He, Y.A. / Jacques, S.L. / Lunney, E.A. / McTigue, M. / Molina, D. / Quenzer, T. / Wells, P.A. / Yu, X. / Zhang, Y. / Zou, A. / Emmett, M.R. / Marshall, A.G. / Zhang, H.M. / Demetri, G.D.
External linksProc. Natl. Acad. Sci. USA / PubMed:19164557
MethodsX-ray diffraction
Resolution1.6 - 2.6 Å
Structure data

PDB-3g0e:
KIT kinase domain in complex with sunitinib
Method: X-RAY DIFFRACTION / Resolution: 1.6 Å

PDB-3g0f:
KIT kinase domain mutant D816H in complex with sunitinib
Method: X-RAY DIFFRACTION / Resolution: 2.6 Å

Chemicals

ChemComp-B49:
N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carbo / medication, anticancer, inhibitor*YM

ChemComp-HOH:
WATER

ChemComp-SO4:
SULFATE ION

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / KIT Kinase domain / Sutent binding / drug resistance / ATP-binding / Disease mutation / Glycoprotein / Immunoglobulin domain / Kinase / Membrane / Nucleotide-binding / Phosphoprotein / Polymorphism / Proto-oncogene / Receptor / Transmembrane / Tyrosine-protein kinase

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