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TitlePonatinib Inhibits Polyclonal Drug-Resistant KIT Oncoproteins and Shows Therapeutic Potential in Heavily Pretreated Gastrointestinal Stromal Tumor (GIST) Patients.
Journal, issue, pagesClin. Cancer Res., Vol. 20, Page 5745-5755, Year 2014
Publish dateJul 11, 2014 (structure data deposition date)
AuthorsGarner, A.P. / Gozgit, J.M. / Anjum, R. / Vodala, S. / Schrock, A. / Zhou, T. / Serrano, C. / Eilers, G. / Zhu, M. / Ketzer, J. ...Garner, A.P. / Gozgit, J.M. / Anjum, R. / Vodala, S. / Schrock, A. / Zhou, T. / Serrano, C. / Eilers, G. / Zhu, M. / Ketzer, J. / Wardwell, S. / Ning, Y. / Song, Y. / Kohlmann, A. / Wang, F. / Clackson, T. / Heinrich, M.C. / Fletcher, J.A. / Bauer, S. / Rivera, V.M.
External linksClin. Cancer Res. / PubMed:25239608
MethodsX-ray diffraction
Resolution2 Å
Structure data

PDB-4u0i:
Crystal structure of KIT in complex with ponatinib
Method: X-RAY DIFFRACTION / Resolution: 2 Å

Chemicals

ChemComp-0LI:
3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzam / medication*YM

ChemComp-PO4:
PHOSPHATE ION

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/TRANSFERASE INHIBITOR / KIT / receptor tyrosine kinase / inhibitor / ponatinib / TRANSFERASE-TRANSFERASE INHIBITOR complex

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