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TitleA model for decoding resistance in precision oncology: acquired resistance to FGFR inhibitors in cholangiocarcinoma.
Journal, issue, pagesAnn Oncol, Vol. 36, Page 426-443, Year 2025
Publish dateFeb 21, 2024 (structure data deposition date)
AuthorsGoyal, L. / DiToro, D. / Facchinetti, F. / Martin, E.E. / Peng, P. / Baiev, I. / Iyer, R. / Maurer, J. / Reyes, S. / Zhang, K. ...Goyal, L. / DiToro, D. / Facchinetti, F. / Martin, E.E. / Peng, P. / Baiev, I. / Iyer, R. / Maurer, J. / Reyes, S. / Zhang, K. / Majeed, U. / Berchuck, J.E. / Chen, C.T. / Walmsley, C. / Pinto, C. / Vasseur, D. / Gordan, J.D. / Mody, K. / Borad, M. / Karasic, T. / Damjanov, N. / Danysh, B.P. / Wehrenberg-Klee, E. / Kambadakone, A.R. / Saha, S.K. / Hoffman, I.D. / Nelson, K.J. / Iyer, S. / Qiang, X. / Sun, C. / Wang, H. / Li, L. / Javle, M. / Lin, B. / Harris, W. / Zhu, A.X. / Cleary, J.M. / Flaherty, K.T. / Harris, T. / Shroff, R.T. / Leshchiner, I. / Parida, L. / Kelley, R.K. / Fan, J. / Stone, J.R. / Uboha, N.V. / Hirai, H. / Sootome, H. / Wu, F. / Bensen, D.C. / Hollebecque, A. / Friboulet, L. / Lennerz, J.K. / Getz, G. / Juric, D.
External linksAnn Oncol / PubMed:39706336
MethodsX-ray diffraction
Resolution2.04 - 2.98 Å
Structure data

PDB-8w2x:
TAS-120 covalent structure with FGFR2
Method: X-RAY DIFFRACTION / Resolution: 2.98 Å

PDB-8w38:
TAS-120 covalent structure with FGFR2 molecular brake mutant
Method: X-RAY DIFFRACTION / Resolution: 2.6 Å

PDB-8w3b:
TAS-120 covalent structure with FGFR2 molecular brake mutant
Method: X-RAY DIFFRACTION / Resolution: 2.23 Å

PDB-8w3d:
TAS-120 covalent structure with FGFR2 molecular brake mutant
Method: X-RAY DIFFRACTION / Resolution: 2.04 Å

Chemicals

PDB-1afr:
STEAROYL-ACYL CARRIER PROTEIN DESATURASE FROM CASTOR SEEDS

ChemComp-GOL:
GLYCEROL

ChemComp-SO4:
SULFATE ION

ChemComp-HOH:
WATER

ChemComp-TZ0:
1-[(3S)-3-{4-amino-3-[(3,5-dimethoxyphenyl)ethynyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl}pyrrolidin-1-yl]prop-2-en-1-one

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/TRANSFERASE INHIBITOR / FGFR2 / TAS-120 / inhibitor / complex / TRANSFERASE / TRANSFERASE-Transferase Inhibitor complex / Kinase / Molecular Brake / transferase inhibitor complex / transferase-inhibitor complex

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