Article
Biochemistry & Molecular Biology
Candice B. Herber, Chaoshen Yuan, Anthony Chang, Jen-Chywan Wang, Isaac Cohen, Dale C. Leitman
Summary: This study suggests that 2',3',4'-THC may act as a new class of ERα modulators that are not direct agonists or antagonists. By altering the activity of ERα on gene regulation and cell proliferation, 2',3',4'-THC has a reprogramming effect, unlike antagonists that compete with E2 for binding to ERα. Adding a reprogramming drug to MHT may offer a new strategy to overcome the adverse proliferative effects of estrogen in MHT.
MOLECULAR MEDICINE
(2022)
Article
Pharmacology & Pharmacy
Yi Jing, Tianhui Hu, Jun Yuan, Zhikun Liu, Mingtao Tao, Mingyu Ou, Xinru Cheng, Wei Cheng, Yuanyuan Yi, Qingping Xiong
Summary: This study demonstrates that resveratrol reduces PCSK9 expression in hepatocytes through ER alpha-mediated signaling, which leads to a decrease in dyslipidemia and aortic plaque area in postmenopausal AS.
BIOCHEMICAL PHARMACOLOGY
(2023)
Article
Endocrinology & Metabolism
Aylin Del Moral-Morales, Juan Carlos Gonzalez-Orozco, Ana Maria Hernandez-Vega, Karina Hernandez-Ortega, Karla Mariana Pena-Gutierrez, Ignacio Camacho-Arroyo
Summary: A study found that in human Glioblastomas (GBM), the pro-oncogenic actions of 17 beta-estradiol (E2) are mediated by EZH2, which promotes proliferation, migration, and invasion of GBM cells. Although E2 does not modify EZH2 expression, gene silencing and pharmacological inhibition of EZH2 can block these pro-oncogenic actions.
FRONTIERS IN ENDOCRINOLOGY
(2022)
Review
Oncology
Nivida Shete, Jordan Calabrese, Debra A. Tonetti
Summary: Estrogen is a key driver of estrogen-receptor-positive breast cancers, and drugs that block estrogen signaling are commonly used for treatment. Surprisingly, estrogen was previously used to treat breast cancer before the introduction of tamoxifen. This review focuses on the insights, molecular mechanisms, and potential clinical application of this counterintuitive therapeutic approach.
Article
Biochemistry & Molecular Biology
Taija Heinosalo, Kalle T. Rytkonen, Niina Saarinen, Paivi Jarvensivu, Pauliina Damdimopoulou, Leena Strauss, Satu Orasniemi, Petricia Horshauge, Michael Gabriel, Pasi Koskimies, Claes Ohlsson, Pauliina Kronqvist, Matti Poutanen
Summary: The over-expression of HSD17B1 in TG mice leads to adenomyotic changes, which can be reversed by HSD17B1 inhibitor treatment. Therefore, HSD17B1 is a potential novel drug target for adenomyosis.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Endocrinology & Metabolism
Erzsebet Kovesdi, Ildiko Udvaracz, Angela Kecskes, Szilard Szocs, Szidonia Farkas, Peter Faludi, Tibor Z. Janosi, Istvan M. Abraham, Gergely Kovacs
Summary: In this study, the acute effect of 17 beta-estradiol on the function of striatal cholinergic neurons in adult mice was examined in vitro. The expression of estrogen receptors ER alpha, ER beta, and GPER1 mRNA was found to be low in some striatal cholinergic neurons. High dose of 17 beta-estradiol affected the spontaneous firing rate of these neurons only in old males, while low concentration did not show any acute effect or association with estrus cycle or sex.
FRONTIERS IN ENDOCRINOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Mio Fukuda, Yo Tojo, Ami Sato, Hiroko Saito, Akira Nakanishi, Yoshio Miki
Summary: Germline mutations in the BRCA2 gene are associated with hereditary breast cancer, with BRCA2 playing a role in DNA damage repair during the S phase of the cell cycle. The exact mechanism of BRCA2 in estrogen induction remains unclear.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2022)
Article
Biochemistry & Molecular Biology
Guoshun Luo, Xinyu Li, Xin Lin, Xiang Lu, Zhenbang Li, Hua Xiang
Summary: Endocrine therapy-resistant breast cancer can be overcome by using PROTACs to induce ER alpha degradation. The study describes the design and synthesis of novel ER alpha-targeting PROTACs, and identifies a potent compound 15b that can degrade ER alpha and inhibit breast cancer cell growth.
JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY
(2022)
Article
Endocrinology & Metabolism
Dandan Song, Huan He, Rajitha Indukuri, Zhiqiang Huang, Lina Stepanauskaite, Indranil Sinha, Lars-Arne Haldosen, Chunyan Zhao, Cecilia Williams
Summary: This study investigates the differences between estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ) in regulating cell proliferation and migration. The results show that ERα and ERβ have opposite effects on cell proliferation and different impacts on migration. Furthermore, they regulate distinct sets of target genes, providing valuable insights into the mechanisms of these two different ER isoforms.
FRONTIERS IN ENDOCRINOLOGY
(2022)
Article
Cell Biology
Qiancheng Shi, Ning Liu, Lei Yang, Yi Chen, Yanwen Lu, Hongqian Guo, Xiaodong Han, Dongmei Li, Weidong Gan
Summary: This study demonstrates that E2 amplifies TOP2 beta-mediated TFE3 breaks through ER alpha-dependent pathway in Xp11.2 tRCC, and E2 upregulates TFE3 by NRF1 to increase the risk of TFE3 breaks. E2 is identified as an important pathogenic factor for Xp11.2 tRCC pathogenesis.
CELL COMMUNICATION AND SIGNALING
(2021)
Article
Behavioral Sciences
Christiana K. Miller, John Meitzen
Summary: This study investigates the modulation of anxiety-related and locomotor behaviors in female rodents by the sex steroid hormone 17 beta-estradiol (estradiol) and its Estrogen Receptors (ERs). The results suggest that estradiol mitigates anxiety-related behaviors through activating Estrogen Receptor (ER) beta and increases locomotor behaviors through ER alpha. However, the influence of ERs on these behaviors cannot always be detected.
HORMONES AND BEHAVIOR
(2023)
Article
Chemistry, Medicinal
Ka-Ying Wong, Tsz-Hung Kong, Christina Chui-Wa Poon, Wenxuan Yu, Liping Zhou, Man-Sau Wong
Summary: In this study, the role of ER-α66, ER-α36, and GPER in bone metabolism following icariin treatment was investigated. It was found that icariin regulated ER-α36 and GPER protein expression in osteoblasts by downregulating them and upregulating ER-α66. ER-α36 and GPER acted as negative regulators of ER-α66 in intact osteoblasts.
PHYTOTHERAPY RESEARCH
(2023)
Review
Biology
Amani A. Mahbub
Summary: Several epidemiological studies have suggested that the use of female sex steroid hormones can reduce the risk of colon cancer. This review summarizes the available data on the effects of estradiol and progesterone treatments in male and female in vitro and in vivo models of colon cancer, along with their potential molecular mechanisms. The studies showed that estradiol treatment and activation of its beta receptor inhibited cell proliferation, induced cell cycle arrest, and promoted apoptosis through molecular pathway modulation. Similarly, the inhibition of the alpha receptor also had antitumorigenic effects. Limited studies on progesterone revealed promising tumoricidal actions. Furthermore, the combination of estradiol and progesterone showed enhanced anticancer activities compared to monotherapy. Overall, these studies suggest that female sex steroid hormones could be a novel and effective therapeutic strategy against colon cancer.
Article
Immunology
Lichao Han, Xingzhao Ji, Xueping Liu, Shuai Xu, Fang Li, Yanlin Che, Xiaotong Qiu, Lina Sun, Zhenjun Li
Summary: Males are more susceptible to Nocardia infection, but estrogen promotes bacterial survival and leads to aggravated inflammation in females.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Veterinary Sciences
Hayder Mohammed Hassan Habeeb, Logan Kleditz, Timothy Hazzard, Cecily Bishop, Fred Stormshak, Michelle Anne Kutzler
Summary: The study aimed to evaluate the effect of PG-600 treatment on ESR1 expression in the ovine endometrium during early diestrus. Results showed that progesterone concentrations were significantly higher in the PG-600-treated group on day 7, while ESR1 concentration was significantly reduced. Therefore, although PG-600 may affect progesterone levels, it is unlikely to impair reproductive potential.
VETERINARY MEDICINE AND SCIENCE
(2023)
Article
Biochemistry & Molecular Biology
Hui-Ting Huang, Shun-Fen Tzeng
Summary: Our study demonstrates the role of interleukin-33 (IL-33) in a demyelinating mouse model induced by cuprizone (CPZ), showing that IL-33 can alleviate the reduction of APC+ OLs and the decline of IL-33 levels in the corpus callosum, and promote the expression of myelin basic protein (MBP).
NEUROCHEMISTRY INTERNATIONAL
(2024)
