A novel series of isoindoledione based compounds were identified as potent antagonists of the androgen receptor (AR). SAR around this series revealed dramatic differences in binding and function in mutant variants (MT) of the AR as compared to the wild type (WT) receptor. Optimization of the aniline portion revealed substitution patterns, which yielded potent antagonist activity against the WT AR as well as the MT AR found in the LNCaP and PCa2b human prostate tumor cell lines.
Progesterone receptor is one of the markers used in antibody-based immunohistochemistry for the diagnostics of breast cancer. The shortcomings of antibodies raise the need to focus on alternative molecular recognition. Aptamers are chosen due to their many advantages as compared to antibodies.
As a novel organophosphate ester (NOPE), tris(2,4-di-butylphenyl) phosphate (TDtBPP) has attracted significant attention due to its unexpectedly high detection in natural environments. However, the ecological toxic effects of environmentally relevant concentrations of TDtBPP in organisms remain entirely unknown. In this study, 1 month old zebrafish were exposed to 0, 50, 500, or 5000 ng/L TDtBPP for 150 days, and the reproductive toxicity in male fish was evaluated.
Stage-specific embryonic antigen-4 (SSEA-4) is a developmentally regulated antigen, while expression level of SSEA-4 and / or its synthase ST3GAL2 is associated with prognosis in various malignancies. We have reported a prominent increase of SSEA-4 in castration-resistant prostate cancer (CRPC) and its negative correlation with the androgen receptor (AR). Meanwhile, loss of AR has increased to approximately 30% with the growing use of androgen receptor signaling inhibitor for metastatic CRPC (mCRPC).
Department of Biological Sciences, Institute of Biosciences, Humanities and Exact Sciences, São Paulo State University (UNESP), São José do Rio Preto, São Paulo, Brazil.
Background: Benign prostatic hyperplasia (BPH) is a disease linked to the hormonal imbalance that occurs during aging and over the last decades, complementary and alternative medicines have come on the scene as a treatment option for BPH, such as herbal medicines. Coconut oil has been shown to be capable of interfering in testosterone-induced BPH. However, until now there is no study of the effect of coconut oil during aging.
Testosterone signaling mediates diseases such as androgenetic alopecia and prostate cancer and is controlled by the activation of the androgen receptor (AR) and nuclear translocation of the ligand-receptor complex. This study established an immortalized dermal papilla cell line that stably expresses the AR labeled with a monomeric green fluorescence marker. The cells expressed the histone H2B protein as visualized using a red fluorescence marker, enabling the Detection of nuclear translocation under live cell conditions using image analysis.
