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Low-molecular-weight Ligand of the Thyroid-stimulating Hormone Receptor with the Activity of a Partial Agonist and a Negative Allosteric Modulator.
Dokl Biochem Biophys
January 2025
I.M. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, St. Petersburg, Russia.
Graves' disease is caused by overactivation of the thyroid-stimulating hormone receptor (TSHR). One approach for its treatment may be the use of negative allosteric modulators (NAM) of TSHR, which normalize TSHR activity and do not cause thyroid hormone (TH) deficiency. The aim of the work was to study the effect of a new compound 5-amino-4-(4-bromophenyl)-2-(methylthio)thieno[2,3-d]pyrimidine-6-carboxylic acid N-tert-butylamide (TPY4) on the basal and TSH-stimulated TH production in cultured FRTL-5 thyrocytes and on basal and thyrotropin-releasing hormone (TRH)-stimulated TH levels in the blood of rats.
View Article and Find Full Text PDFA Narrative Review of Cardiometabolic Profiles among U.S. Adults: Temporal Trends and Implications.
Curr Cardiol Rep
January 2025
John Ochsner Heart and Vascular Institute, Ochsner Clinical School University of Queensland School of Medicine, New Orleans, LA, USA.
Purpose Of Review: To provide a narrative overview of trends and disparities in the cardiometabolic profiles of U.S. adults by synthesizing findings from nationally representative studies conducted between 1999 and 2020.
View Article and Find Full Text PDFAttenuating hyperammonemia preserves protein synthesis and muscle mass via restoration of perturbed metabolic pathways in bile duct-ligated rats.
Metab Brain Dis
January 2025
Hepato-Neuro Laboratory, Centre Hospitalier de l'Université de Montréal (CRCHUM), Université de Montréal, 900, Rue Saint-Denis - Pavillon R, R08.422, Montréal (Québec), H2X 0A9, Canada.
Sarcopenia and hepatic encephalopathy (HE) are complications of chronic liver disease (CLD), which negatively impact clinical outcomes. Hyperammonemia is considered to be the central component in the pathogenesis of HE, however ammonia's toxic effects have also been shown to impinge on extracerebral organs including the muscle. Our aim was to investigate the effect of attenuating hyperammonemia with ornithine phenylacetate (OP) on muscle mass loss and associated molecular mechanisms in rats with CLD.
View Article and Find Full Text PDFMicrovascular reconstruction in oral and maxillofacial surgery: a Europe-wide data collection.
Oral Maxillofac Surg
January 2025
Department of Oral and Maxillofacial Surgery, German Armed Forces Central Hospital, Rübenacherstr. 170, 56072, Koblenz, Germany.
Purpose: This study aims to analyze microvascular reconstruction in Oral and Maxillofacial Surgery (OMFS) in Europe.
Methods: Based on previous studies, a dynamic online questionnaire was developed and subjected to internal and external evaluation. The questionnaire comprised multiple-choice, rating, and open-ended questions, addressing general and specific aspects and the impacts of the COVID-19 pandemic on microvascular reconstruction in OMFS in Europe.
Active targeting of type 1 diabetes therapies to pancreatic beta cells using nanocarriers.
Diabetologia
January 2025
Department of Chemical and Biological Engineering, Colorado School of Mines, Golden, CO, USA.
Type 1 diabetes is an autoimmune disease characterised by the destruction of pancreatic beta cells, resulting in lifelong insulin dependence. Although exogenous insulin can maintain glycaemic control, this approach does not protect residual or replacement pancreatic beta cells from immune-mediated death. Current therapeutics designed to protect functional beta cell mass or promote beta cell proliferation and regeneration can have off-target effects, resulting in higher dose requirements and adverse side effects.
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