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Identification, structure, and agonist design of an androgen membrane receptor.
Cell
January 2025
Key Laboratory Experimental Teratology of the Ministry of Education, New Cornerstone Science Laboratory, Department of Biochemistry and Molecular Biology, School of Basic Medical Sciences, and Advanced Medical Research Institute, NHC Key Laboratory of Otorhinolaryngology, Qilu hospital, Cheeloo College of Medicine, Shandong University, Jinan 250012, China; Department of Physiology and Pathophysiology, School of Basic Medical Sciences, State Key Laboratory of Vascular Homeostasis and Remodeling, Beijing Key Laboratory of Cardiovascular Receptors Research, Peking University, Beijing 100191, China. Electronic address:
Androgens, such as 5α-dihydrotestosterone (5α-DHT), regulate numerous functions by binding to nuclear androgen receptors (ARs) and potential unknown membrane receptors. Here, we report that the androgen 5α-DHT activates membrane receptor GPR133 in muscle cells, thereby increasing intracellular cyclic AMP (cAMP) levels and enhancing muscle strength. Further cryoelectron microscopy (cryo-EM) structural analysis of GPR133-Gs in complex with 5α-DHT or its derivative methenolone (MET) reveals the structural basis for androgen recognition.
View Article and Find Full Text PDFPrevalence and predictive factors of testosterone-induced erythrocytosis: a retrospective single center study.
Front Endocrinol (Lausanne)
January 2025
Department of Internal Medicine, Division of Endocrinology, Diabetes and Clinical Nutrition, Luzerner Kantonsspital, Lucerne, Switzerland.
Aim: This study analyzes the prevalence and predictive factors of testosterone-induced erythrocytosis (TIE) in patients receiving testosterone replacement therapy (TRT).
Methods: Retrospective single-center observational study.
Results: 247 patients were included; median age was 47.
Application of the Integrated Approach to Testing and Assessment (IATA) for evaluating endocrine disruption potential of selected pyrethroids by H295R steroidogenesis and ER/AR transcriptional activation.
Chemosphere
January 2025
College of Pharmacy, Dongduk Women's University, Seoul, 02748, South Korea. Electronic address:
Pyrethroids, which are widely utilized in agriculture, household products, and public health for their potent insecticidal properties, elicit significant concerns regarding their potential endocrine-disrupting effects. However, previous studies have yielded inconsistent data, largely due to the absence of a standardized screening system. To address this limitation, the present study introduces an Integrated Approach to Testing and Assessment (IATA) to evaluate the endocrine-disrupting potential of pyrethroids, aligned with the Adverse Outcome Pathway (AOP) framework.
View Article and Find Full Text PDFEstablishment of Rat Models Mimicking Gender-affirming Hormone Therapies.
J Vis Exp
January 2025
Center for Gender-Specific Medicine, Istituto Superiore di Sanità.
Transgender (TG) people are individuals whose gender identity and sex assigned at birth do not match. They often undergo gender-affirming hormone therapy (GAHT), a medical intervention that allows the acquisition of secondary sex characteristics more aligned with their individual gender identity, providing consistent results in the improvement of numerous socio-psychological variables. However, GAHT targets different body systems, and some side effects are recorded, although not yet fully identified and characterized.
View Article and Find Full Text PDFOral and topical spironolactone in acne treatment: A meta-analysis of effectiveness and safety.
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Faculty of Medicine, Cairo University, Cairo, Egypt.
Acne vulgaris (AV) is a common chronic inflammatory skin disorder that commonly lasts from adolescence to adulthood and has serious social and psychological consequences. Current treatments typically use antibacterial drugs, which contributes to the rise in antibacterial drug resistance. Spironolactone, a potassium-sparing diuretic with anti-androgen effects, has been used off-label to treat acne by lowering sebum production.
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