13 results found
    1. Cancer Biology

    TLE3 loss confers AR inhibitor resistance by facilitating GR-mediated human prostate cancer cell growth

    Sander AL Palit et al.
    A mechanistic link between TLE3 loss and glucocorticoid receptor-mediated androgen receptor inhibitor resistance supports the rationale to target GR during anti-hormonal treatment in castrate-resistant prostate cancer.
    1. Cancer Biology

    GREB1 amplifies androgen receptor output in human prostate cancer and contributes to antiandrogen resistance

    Eugine Lee et al.
    Prostate cancer cells maintain heterogeneous androgen receptor transcriptional activity through upregulation of AR-regulated coactivator GREB1, and cells with high activity rapidly develop resistance to antiandrogen therapy in a GREB1-dependent manner.
    1. Biochemistry and Chemical Biology
    2. Cancer Biology

    Aberrant corticosteroid metabolism in tumor cells enables GR takeover in enzalutamide resistant prostate cancer

    Jianneng Li et al.
    Prostate cancer resistance to androgen receptor antagonist therapy occurs by way of tumors impeding local glucocorticoid metabolism and inactivation and thereby permitting sustained glucocorticoids to stimulate up-regulated glucocorticoid receptor.
    1. Cancer Biology

    Overcoming mutation-based resistance to antiandrogens with rational drug design

    Minna D Balbas et al.
    Mutagenesis studies identified an androgen receptor mutation that converts enzalutamide-a drug recently approved for the treatment of advanced prostate cancer-into an androgen receptor agonist, and modeling studies informed the design of novel drugs that are effective against the mutant receptor.
    1. Cancer Biology

    Regulation of the glucocorticoid receptor via a BET-dependent enhancer drives antiandrogen resistance in prostate cancer

    Neel Shah et al.
    Epigenetic regulation of the glucocorticoid receptor in castration-resistant prostate cancer can be targeted via the use of BET bromodomain inhibitors.
    1. Cancer Biology

    Human DECR1 is an androgen-repressed survival factor that regulates PUFA oxidation to protect prostate tumor cells from ferroptosis

    Zeyad D Nassar et al.
    DECR1, a rate-limiting enzyme for polyunsaturated fatty acid (PUFA) β-oxidation, is an androgen-repressed gene in prostate cancer cells that limits oxidative stress to promote cancer cell survival.
    1. Cancer Biology

    Cancer: Designer antiandrogens join the race against drug resistance

    Jatinder S Josan, John A Katzenellenbogen
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    1. Cancer Biology

    The identification of dual protective agents against cisplatin-induced oto- and nephrotoxicity using the zebrafish model

    Jaime N Wertman et al.
    L-mimosine and dopamine protect against cisplatin-induced oto- and nephrotoxicity in zebrafish and human cell line models.
    1. Biochemistry and Chemical Biology
    2. Cancer Biology

    AR phosphorylation and CHK2 kinase activity regulates IR-stabilized AR–CHK2 interaction and prostate cancer survival

    Huy Q Ta et al.
    CHK2 directly binds the AR to mediate transient suppression of AR activity and thus loss of CHK2 function in prostate cancer increases AR activity, DNA damage response and radiation resistance.
    1. Cancer Biology

    Development of Bag-1L as a therapeutic target in androgen receptor-dependent prostate cancer

    Laura Cato et al.
    Targeting the activation of the androgen receptor N-terminal domain by the cochaperone Bag-1L provides a new approach for inhibiting androgen receptor function to treat prostate cancer.

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