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    BIOMARKER:

    MET Y1230C

    i
    Other names: DFNB97, AUTS9, RCCP2, C-Met, HGFR, HGF Receptor, Met Proto-Oncogene, HGF/SF Receptor, Proto-Oncogene C-Met, Scatter Factor Receptor, Tyrosine-Protein Kinase Met, Hepatocyte Growth Factor Receptor, MET, MET Proto-Oncogene, Receptor Tyrosine Kinase
    Entrez ID:
    4233
    Related biomarkers:
    Expression
    Mutation
    CNA
    Fusion
    Others
    12ms
    Structural insight into the macrocyclic inhibitor TPX-0022 of c-Met and c-Src. (PubMed, Comput Struct Biotechnol J)
    In addition, TPX-0022 exhibited potent activity against the resistance-relevant c-Met L1195F mutant and moderate activity against the c-Met G1163R, F1200I and Y1230H mutants but weak activity against the c-Met D1228N and Y1230C mutants. Overall, our study reveals the structural mechanism underlying the potency and selectivity of TPX-0022 and the ability to overcome acquire resistance mutations and provides insight into the development of selective c-Met macrocyclic inhibitors.
    Journal
    |
    MET (MET proto-oncogene, receptor tyrosine kinase) • CSF1R (Colony stimulating factor 1 receptor)
    |
    MET mutation • MET D1228N • MET F1200I • MET Y1230C • MET Y1230C
    |
    elzovantinib (TPX-0022)
    12ms
    Biophysical and structural characterization of the impacts of MET phosphorylation on tepotinib binding. (PubMed, J Biol Chem)
    We corroborated these data with target engagement studies by fluorescence cross-correlation spectroscopy using KD constructs in cell lysates or full-length receptors from solubilized cellular membranes as wildtype or activated mutants (Y1235D and Y1234E/1235E). Collectively, our results provide further insight into the MET A-loop structural determinants that affect the binding of the selective inhibitor tepotinib.
    Journal
    |
    HGF (Hepatocyte growth factor)
    |
    MET F1200I • MET Y1230C • MET Y1230C
    |
    Tepmetko (tepotinib)
    over1year
    Predictive Biomarkers of Response to REGN5093 to Guide Patient Selection in MET-Altered Advanced Non-small Cell Lung Cancer (IASLC-WCLC 2023)
    We report biomarkers associated with clinical response and resistance to REGN5093 which may help with screening of aNSCLC pts in future combination studies of REGN5093 with other therapies.
    Clinical • Metastases
    |
    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • TP53 (Tumor protein P53) • JAK2 (Janus kinase 2)
    |
    EGFR mutation • BRAF mutation • MET amplification • KRAS G12D • PIK3CA H1047R • MET exon 14 mutation • MET overexpression • MET mutation • MET expression • KRAS G12 • JAK2 V617F • TP53 R248Q • EGFR mutation + MET-CEP7 fusion • MET Y1230C • MET D1228H • MET Y1230C
    |
    FoundationOne® CDx • TruSight Oncology 500 Assay
    |
    davutamig (REGN5093)