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The L730V/I RET roof mutations display different activities toward pralsetinib and selpercatinib.


ABSTRACT: Recently Food and Drug Administration (FDA)-approved pralsetinib (BLU-667) and selpercatinib (LOXO-292) are RET-selective protein tyrosine kinase inhibitors for treating RET-altered cancers, but whether they have distinct activity was unknown. The L730V/I mutations at the roof of the solvent-front site of the RET kinase were identified as strongly resistant to pralsetinib but not to selpercatinib. Selpercatinib effectively inhibited these mutants and the KIF5B-RET(L730V/I) oncogene-driven tumors.

SUBMITTER: Shen T 

PROVIDER: S-EPMC8184971 | biostudies-literature |

REPOSITORIES: biostudies-literature

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