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    BIOMARKER:

    AR W741C

    i
    Other names: AR, AIS, DHTR, HUMARA, NR3C4, SBMA, SMAX1, Androgen receptor
    Entrez ID:
    367
    Related biomarkers:
    Expression
    Mutation
    CNA
    Others
    1m
    Identification of Oral Bioavailable Coumarin Derivatives as Potential AR Antagonists Targeting Prostate Cancer. (PubMed, J Med Chem)
    Especially, 4a showed superior efficacy against ARF876L/T877A and ARW741C mutants compared to darolutamide and enzalutamide. Moreover, 4a exhibited favorable pharmacokinetic profiles (F = 66.24%) in vivo and significant tumor growth inhibition in an LNCaP xenograft mouse model upon oral administration. These results highlight the potential of 4a as a promising oral AR antagonist for overcoming drug resistance in PCa.
    Journal
    |
    AR (Androgen receptor)
    |
    AR F876L • AR T877A • AR W741C
    |
    Xtandi (enzalutamide) • Nubeqa (darolutamide)