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TitleCharacterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397.
Journal, issue, pagesCancer Discov, Vol. 5, Page 668-679, Year 2015
Publish dateNov 13, 2014 (structure data deposition date)
AuthorsSmith, C.C. / Zhang, C. / Lin, K.C. / Lasater, E.A. / Zhang, Y. / Massi, E. / Damon, L.E. / Pendleton, M. / Bashir, A. / Sebra, R. ...Smith, C.C. / Zhang, C. / Lin, K.C. / Lasater, E.A. / Zhang, Y. / Massi, E. / Damon, L.E. / Pendleton, M. / Bashir, A. / Sebra, R. / Perl, A. / Kasarskis, A. / Shellooe, R. / Tsang, G. / Carias, H. / Powell, B. / Burton, E.A. / Matusow, B. / Zhang, J. / Spevak, W. / Ibrahim, P.N. / Le, M.H. / Hsu, H.H. / Habets, G. / West, B.L. / Bollag, G. / Shah, N.P.
External linksCancer Discov / PubMed:25847190
MethodsX-ray diffraction
Resolution3.1 Å
Structure data

PDB-4rt7:
Crystal Structure of FLT3 with a small molecule inhibitor
Method: X-RAY DIFFRACTION / Resolution: 3.1 Å

Chemicals

ChemComp-P30:
1-(5-tert-butyl-1,2-oxazol-3-yl)-3-(4-{7-[2-(morpholin-4-yl)ethoxy]imidazo[2,1-b][1,3]benzothiazol-2-yl}phenyl)urea / medication, anticancer, inhibitor*YM

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/TRANSFERASE INHIBITOR / Kinase / TRANSFERASE / TRANSFERASE INHIBITOR / COMPLEX / TRANSFERASE-TRANSFERASE INHIBITOR complex

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