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    BIOMARKER:

    AR F876L

    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)
    over2years
    Conformational dynamics of androgen receptors bound to agonists and antagonists. (PubMed, Sci Rep)
    Principal component analysis (PCA) of the structural fluctuations shows that the binding of enzalutamide and apalutamide induce conformational fluctuations in the AR, which are markedly different from those caused by the agonist as well as another antagonist, bicalutamide. These fluctuations could only be observed with the use of aMD.
    Journal
    |
    AR (Androgen receptor)
    |
    AR F876L
    |
    Xtandi (enzalutamide capsule) • bicalutamide • Erleada (apalutamide)
    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