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    BIOMARKER:

    AR W741L

    i
    Other names: AR, AIS, DHTR, HUMARA, NR3C4, SBMA, SMAX1, Androgen receptor
    Entrez ID:
    367
    Related biomarkers:
    Expression
    Mutation
    CNA
    Others
    over1year
    Design, Synthesis, and Biological Evaluation of Androgen Receptor Degrading and Antagonizing Bifunctional Steroidal Analogs for the Treatment of Advanced Prostate Cancer. (PubMed, J Med Chem)
    Herein, systemic structural modifications on the C-3, C-6, and C-17 positions of galeterone led to the discovery of 67-b with the dual functions of AR antagonism and degradation. In vivo, 67-b effectively inhibited the growth of hormone-sensitive organs in the Hershberger assay and exhibited tumor regression in the enzalutamide-resistant (c4-2b-ENZ) xenograft model. These results confirmed 67-b to be a promising AR degrader and antagonist for the treatment of mCRPC patients.
    Journal
    |
    AR (Androgen receptor)
    |
    AR F876L • AR T877A • AR W741L
    |
    Xtandi (enzalutamide capsule) • galeterone (TOK-001)
    2years
    An insight about the mechanism of action (MoA) of R-bicalutamide on the androgen receptor homodimer using molecular dynamic. (PubMed, Toxicol Appl Pharmacol)
    The results obtained indicate that the binding of R-bicalutamide in the two AR monomers induces a great instability in the homodimer, which may determine the monomer's dissociation preventing AR migration into the nucleus and avoiding the transcriptional activity. If the W741L mutation occurs, the homodimer tends to have a behaviour close to the agonistic system where the two monomers are tightly bound, which may explain the effect of the W741L in drug insensitivity from a structural point of view.
    Journal
    |
    AR (Androgen receptor)
    |
    AR mutation • AR wild-type • AR W741L
    |
    bicalutamide
    over3years
    Design, Synthesis and Evaluation of Novel Substituted (5-methyl-1H-pyrazol-3-yl)-1,3,4-oxadiazole as Potent Androgen Receptor Antagonist. (PubMed, Anticancer Agents Med Chem)
    In this study, we have identified a potential hit molecule for AR antagonism that could be further developed to obtain a potent clinical candidate.
    Journal
    |
    AR (Androgen receptor)
    |
    AR mutation • AR F876L • AR T877A • AR W741L
    |
    Xtandi (enzalutamide capsule) • bicalutamide • flutamide