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TitleStructural basis of acquired resistance to selpercatinib and pralsetinib mediated by non-gatekeeper RET mutations.
Journal, issue, pagesAnn Oncol, Vol. 32, Page 261-268, Year 2021
Publish dateAug 19, 2020 (structure data deposition date)
AuthorsSubbiah, V. / Shen, T. / Terzyan, S.S. / Liu, X. / Hu, X. / Patel, K.P. / Hu, M. / Cabanillas, M. / Behrang, A. / Meric-Bernstam, F. ...Subbiah, V. / Shen, T. / Terzyan, S.S. / Liu, X. / Hu, X. / Patel, K.P. / Hu, M. / Cabanillas, M. / Behrang, A. / Meric-Bernstam, F. / Vo, P.T.T. / Mooers, B.H.M. / Wu, J.
External linksAnn Oncol / PubMed:33161056
MethodsX-ray diffraction
Resolution1.9 - 2.06 Å
Structure data

PDB-7ju5:
Structure of RET protein tyrosine kinase in complex with pralsetinib
Method: X-RAY DIFFRACTION / Resolution: 1.9 Å

PDB-7ju6:
Structure of RET protein tyrosine kinase in complex with selpercatinib
Method: X-RAY DIFFRACTION / Resolution: 2.06 Å

Chemicals

ChemComp-Q4J:
Pralsetinib / medication, inhibitor*YM

ChemComp-FMT:
FORMIC ACID

ChemComp-HOH:
WATER

ChemComp-Q6G:
Selpercatinib / medication, inhibitor*YM

Source
  • homo sapiens (human)
KeywordsTransferase/Transferase inhibitor / oncogene / RET / Tyrosine Kinase / ATP-binding / Thyroid cancer / Non small cell lung cancer / pralsetinib / Transferase-Transferase inhibitor complex / TRANSFERASE / Tyrisine Kinase / ATP binding / LOXO-292 / selpercatinib

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