7JU6

Structure of RET protein tyrosine kinase in complex with selpercatinib

Summary for 7JU6

• Entry DOI: 10.2210/pdb7ju6/pdb
• Descriptor: Proto-oncogene tyrosine-protein kinase receptor Ret, Selpercatinib, FORMIC ACID, ... (4 entities in total)
• Functional Keywords: transferase, oncogene, ret, tyrisine kinase, atp binding, thyroid cancer, non small cell lung cancer, loxo-292, selpercatinib, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 2
• Total formula weight: 72697.80

Authors

Terzyan, S.S.,Shen, T.,Wu, J.,Mooers, B.H.M. (deposition date: 2020-08-19, release date: 2020-11-11, Last modification date: 2023-10-18)

Primary citation

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.
Structural basis of acquired resistance to selpercatinib and pralsetinib mediated by non-gatekeeper RET mutations.
Ann Oncol, 32:261-268, 2021

PubMed Abstract: Selpercatinib (LOXO-292) and pralsetinib (BLU-667) are highly potent RET-selective protein tyrosine kinase inhibitors (TKIs) for treating advanced RET-altered thyroid cancers and non-small-cell lung cancer (NSCLC). It is critical to analyze RET mutants resistant to these drugs and unravel the molecular basis to improve patient outcomes.

PubMed: 33161056
DOI: 10.1016/j.annonc.2020.10.599

Experimental method

X-RAY DIFFRACTION (2.06 Å)