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Estrogen and Androgen Blockade for Advanced Prostate Cancer in the Era of Precision Medicine
Published in Shaker A. Mousa, Raj Bawa, Gerald F. Audette, The Road from Nanomedicine to Precision Medicine, 2020
Tetsuya Fujimura, Kenichi Takayama, Satoru Takahashi, Satoshi Inoue
ERβ activation is a target for treating early stage PC to prevent cancer progression [61, 62]. RNA sequencing and immunohistochemistry were conducted to compare gene expression profiles in the ventral prostate of young (2-month-old) and aging (18-month-old) ERβ/ERβ mice and their wild-type littermates. ERβ modulates AR signaling by repressing AR driver RORc and increasing AR co-repressor dachshund family (DACH 1/2). ERβ loss resulted in the upregulation of genes whose expression is associated with poor prognosis in PC, accompanied with the downregulation of tumor-suppressive or tumor-preventive genes. ERβ agonist (LY3201) treatment resulted in the nuclear import of PTEN and repression of AR signaling.
Estrogen and Androgen Blockade for Advanced Prostate Cancer in the Era of Precision Medicine
Published in Shaker A. Mousa, Raj Bawa, Gerald F. Audette, The Road from Nanomedicine to Precision Medicine, 2019
Tetsuya Fujimura, Kenichi Takayama, Satoru Takahashi, Satoshi Inoue
ERβ activation is a target for treating early stage PC to prevent cancer progression [61, 62]. RNA sequencing and immunohistochemistry were conducted to compare gene expression profiles in the ventral prostate of young (2-month-old) and aging (18-month-old) ERβ/ERβ mice and their wild-type littermates. ERβ modulates AR signaling by repressing AR driver RORc and increasing AR co-repressor dachshund family (DACH 1/2). ERβ loss resulted in the upregulation of genes whose expression is associated with poor prognosis in PC, accompanied with the downregulation of tumor-suppressive or tumor-preventive genes. ERβ agonist (LY3201) treatment resulted in the nuclear import of PTEN and repression of AR signaling.
The effect of sex hormones on skeletal muscle adaptation in females
Published in European Journal of Sport Science, 2022
Sarah E. Alexander, Alexander C. Pollock, Séverine Lamon
Estrogens and progestogens are the major female hormones. Estrogens are produced by the corpus luteum of the ovary, the placenta and to a lesser extent by adipose and other peripheral tissues, and are responsible for the development, regulation and maintenance of the female reproductive system and secondary sex characteristics (Cui, Shen, & Li, 2013). The major bioactive estrogens are estrone (E1), estradiol (E2), and estriol (E3) (Cui et al., 2013). Progestogens, including the most abundant form progesterone, are primarily produced by the corpus luteum of the ovary and regulate the female menstrual cycle and pregnancy (Taraborrelli, 2015). The specific receptors for estrogens (ER) and progestogens (PR) are also expressed in human skeletal muscle (Ekenros et al., 2017). Unlike androgens and progestogens, which have a single receptor (the AR and the PR), there are multiple ERs found in both the cytosol (ERα and ERβ) and the sarcolemma of myocytes, including the g-protein coupled estrogen receptors (GPER), estrogen receptor-X (ER-X) and Gq-coupled membrane estrogen receptor (Gq-mER). These receptors act together to facilitate the function of female sex hormones in the regulation of muscle mass and contractility. The reason for multiple estrogen receptors in skeletal muscle is unclear but may stem from evolution.
Computational prediction models for assessing endocrine disrupting potential of chemicals
Published in Journal of Environmental Science and Health, Part C, 2018
Sugunadevi Sakkiah, Wenjing Guo, Bohu Pan, Rebecca Kusko, Weida Tong, Huixiao Hong
ER has two major isoforms: ER-α and ER-β. Concentrations of these two types of ER vary between tissues. Chemicals selectively binding to one type of ER are called selective estrogen receptor modulators. Selective estrogen receptor modulators are relevant to drug discovery and safety evaluation.11