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    BIOMARKER:

    KIF5B-RET fusion + RET V804M

    i
    Other names: KIF5B, Kinesin Family Member 5B, Conventional Kinesin Heavy Chain, Ubiquitous Kinesin Heavy Chain, Kinesin-1 Heavy Chain, KNS1, UKHC, KNS, Epididymis Secretory Protein Li 61, Kinesin 1 (110-120kD), Kinesin Heavy Chain, HEL-S-61, KINH, RET, Ret Proto-Oncogene, Proto-Oncogene Tyrosine-Protein Kinase Receptor Ret, Cadherin-Related Family Member 16, Rearranged During Transfection, RET Receptor Tyrosine Kinase, Cadherin Family Member 12, Proto-Oncogene C-Ret, CDHF12, CDHR16, PTC, Ret Proto-Oncogene (Multiple Endocrine Neoplasia And Medullary Thyroid Carcinoma 1, Hirschsprung Disease), Multiple Endocrine Neoplasia And Medullary Thyroid Carcinoma 1, Hirschsprung Disease 1, RET-ELE1, HSCR1, MEN2A, MEN2B, RET51, MTC1
    Entrez ID:
    5979; 3799
    Related biomarkers:
    Expression
    Mutation
    CNA
    Fusion
    Others
    11ms
    Discovery of an Efficacious RET PROTAC Degrader with Enhanced Antiproliferative Activity against Resistant Cancer Cells Harboring RET Solvent-Front Mutations. (PubMed, J Med Chem)
    Although two selective RET inhibitors, selpercatinib and pralsetinib, have been approved by the FDA, acquired resistance through solvent-front mutations has been identified rapidly. Notably, QZ2135 demonstrated in vivo antitumor efficacy in a Ba/F3-KIF5B-RET-G810C xenograft mouse model. Together, this study provides a potential alternative strategy for overcoming acquired resistance to RET inhibitors mediated by solvent-front mutations.
    Journal
    |
    RET (Ret Proto-Oncogene) • KIF5B (Kinesin Family Member 5B)
    |
    RET mutation • RET V804M • KIF5B-RET fusion + RET V804M • RET V804*
    |
    Retevmo (selpercatinib) • Gavreto (pralsetinib)