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About 55,453 results

Dual gut hormone receptor agonists for diabetes and obesity.
https://doi.org/10.1172/JCI167952
The Journal of Clinical Investigation; Bass J, Tschöp MH et. al.

Feb 1st, 2023 - Dual gut hormone receptor agonists for diabetes and obesity.|2023|Bass J,Tschöp MH,Beutler LR,|drug therapy,drug therapy,agonists,

Mechanism of hormone and allosteric agonist mediated activation of follicle stimulating...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9889800
Nature Communications; Duan J, Xu P et. al.

Feb 1st, 2023 - Follicle stimulating hormone (FSH) is an essential glycoprotein hormone for human reproduction, which functions are mediated by a G protein-coupled receptor, FSHR. Aberrant FSH-FSHR signaling causes infertility and ovarian hyperstimulation syndrome. Here we report cryo-EM structures of FSHR in both inactive and active states, with the active structure bound to FSH and an allosteric agonist comp...

Activation of Most Toll-Like Receptors in Whole Human Blood Attenuates Platelet Deposit...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9873445
Journal of Immunology Research; Liu Y, Diamond SL

Jan 28th, 2023 - Platelets have toll-like receptors (TLRs); however, their function in thrombosis or hemostasis under flow conditions is not fully known. Thrombin-inhibited anticoagulated whole blood was treated with various TLR agonists and then perfused over fibrillar collagen using microfluidic assay at venous wall shear rate (100 s-1). Platelet deposition was imaged with fluorescent anti-CD61. For perfusion...

New Frontiers in Obesity Treatment: GLP-1 and Nascent Nutrient-Stimulated Hormone-Based...
https://doi.org/10.1146/annurev-med-043021-014919
Annual Review of Medicine; Jastreboff AM, Kushner RF

Jan 28th, 2023 - Nearly half of Americans are projected to have obesity by 2030, underscoring the pressing need for effective treatments. Glucagon-like peptide 1 receptor agonists (GLP-1 RAs) represent the first agents in a rapidly evolving, highly promising landscape of nascent hormone-based obesity therapeutics. With the understanding of the neurobiology of obesity rapidly expanding, these emerging entero-end...

Effect of glucagon-like peptide-1 receptor agonists on glycemic control, and weight red...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9876280
PloS One; Yeh TL, Tsai MC et. al.

Jan 26th, 2023 - To explore the effect of glucagon-like peptide-1 receptor agonist (GLP-1 RAs) on glycemic control and weight reduction in adults. Databases were searched from August 2021 to March 2022. Data were analyzed using mean difference (MD) values with 95% confidence intervals (CIs). Both random-and fixed-effect models were employed. Heterogeneity was explored using pre-specified subgroup analyses and m...

Glucagon-like peptide-1/glucagon receptor agonism associates with reduced metabolic ada...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9881753
Obesity (Silver Spring, Md.); Corbin KD, Carnero EA et. al.

Jan 26th, 2023 - This study tested the hypothesis that treatment with the glucagon-like peptide-1/glucagon receptor agonist SAR425899 would lead to a smaller decrease in sleeping metabolic rate (SMR; kilocalories/day) than expected from the loss of lean and fat mass (metabolic adaptation). This Phase 1b, double-blind, randomized, placebo-controlled study was conducted at two centers in inpatient metabolic wards...

Efficacy and safety of semaglutide for weight management: evidence from the STEP program.
https://doi.org/10.1080/00325481.2022.2147326
Postgraduate Medicine; Amaro A, Sugimoto D et. al.

Jan 25th, 2023 - Obesity is a global health challenge. It is a multifactorial, complex, and progressive disease associated with various health complications and increased mortality. Lifestyle modifications are central to weight management but may be insufficient to maintain clinically meaningful weight loss. Pharmacotherapies are recommended as an adjunct to lifestyle interventions to induce and sustain clinica...

Structural and dynamic insights into supra-physiological activation and allosteric modu...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9870890
Nature Communications; Xu J, Wang Q et. al.

Jan 24th, 2023 - The M2 muscarinic receptor (M2R) is a prototypical G-protein-coupled receptor (GPCR) that serves as a model system for understanding GPCR regulation by both orthosteric and allosteric ligands. Here, we investigate the mechanisms governing M2R signaling versatility using cryo-electron microscopy (cryo-EM) and NMR spectroscopy, focusing on the physiological agonist acetylcholine and a supra-physi...

Analysis of euploidy rates in preimplantation genetic testing for aneuploidy cycles wit...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9841681
European Journal of Medical Research; Wang L, Wang J et. al.

Jan 16th, 2023 - Progestins can suppress endogenous luteinising hormone (LH) secretion from the pituitary gland and have shown similar efficacy in terms of collecting competent oocytes and embryos; however, some inconsistencies have been proposed regarding the quality of embryos collected with the use of progestins. This study aimed to evaluate euploidy rates and pregnancy outcomes in preimplantation genetic te...

Complement activation negatively affects the platelet response to thrombopoietin recept...
https://doi.org/10.1080/09537104.2022.2159019
Platelets Åkesson A, Bussel JB et. al.

Jan 14th, 2023 - Increased platelet destruction is central in the pathogenesis of immune thrombocytopenia. However, impaired platelet production is also relevant and its significance underlies the rationale for treatment with thrombopoietin receptor agonists (TPO-RAs). Previous studies have associated enhanced complement activation with increased disease severity. Additionally, treatment refractoriness has been...

Impact of PPAR-gamma activation on the durability of biological heart valve prostheses ...
https://doi.org/10.1093/ejcts/ezad005
European Journal of Cardio-thoracic Surgery : Official Jo... Assmann AK, Winnicki V et. al.

Jan 12th, 2023 - Hypercholesterolaemia and obesity are risk factors for the development of calcified aortic valve disease and common comorbidities in respective patients. Peroxisome proliferator-activated receptor gamma activation has been shown to reduce the progression of native aortic valve sclerosis, while its effect on bioprosthetic valve degeneration is yet unknown. This project aims to analyse the impact...

Peroxisome proliferator-activated receptor gamma agonists for preventing recurrent stro...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9830907
The Cochrane Database of Systematic Reviews; Liu J, Wang LN

Jan 11th, 2023 - Peroxisome proliferator-activated receptor gamma (PPAR-γ) agonists are insulin-sensitising drugs used for the treatment of insulin resistance. In addition to lowering glucose in diabetes, these drugs may also protect against hyperlipidaemia and arteriosclerosis, which are risk factors for stroke. This is an update of a review first published in January 2014 and subsequently updated in December ...

Insights into the toxicities of UV-328, UV-329, UV-P in HepG2 cells and their roles in ...
https://doi.org/10.1016/j.ecoenv.2022.114478
Ecotoxicology and Environmental Safety; Liang S, Zhang Y et. al.

Jan 1st, 2023 - The widespread high concentrations of benzotriazole ultraviolet stabilizers (BUVSs) in many biotic and abiotic samples have raised urgent concerns of their adverse effects on environmental and human health. In this study, we investigated the toxicity of three typical BUVSs (UV-328, UV-329, UV-P) with HepG2 cells in vitro. Results indicated that the three BUVSs showed weak cytotoxicity in HepG2 ...

TLR8 agonist partially improves IFN-γ deficiency of NK cells in chronic hepatitis B thr...
https://doi.org/10.1111/apt.17382
Alimentary Pharmacology & Therapeutics; Ao X, Gan Q et. al.

Jan 1st, 2023 - Natural killer (NK) cells exhibit a selective deficiency of IFN-γ production in chronic hepatitis B (CHB). Toll-like receptor 8 (TLR8) agonists could induce IFN-γ production in immune cells, although their effects on the deficiency in NK cells remain unclear. To investigate TLR8 expression in NK cells and the effect of TLR8 agonists in patients with CHB METHODS: We enrolled 32 patients with CHB...

Nonclinical safety assessments of a novel synthetic toll-like receptor 4 agonist and sa...
https://doi.org/10.1016/j.taap.2022.116358
Toxicology and Applied Pharmacology; Syntin P, Piras-Douce F et. al.

Dec 27th, 2022 - A full nonclinical safety package was performed to support the clinical use of SPA14, a novel liposome-based vaccine adjuvant containing the synthetic toll-like receptor 4 agonist E6020 and saponin QS21. E6020 and QS21 were tested negative for their potential genotoxic effects in Ames, micronucleus, or mouse-lymphoma TK (thymidine kinase) assay. To evaluate the potential local and systemic effe...

Glucagon, from past to present: a century of intensive research and controversies.
https://doi.org/10.1016/S2213-8587(22)00349-7
The Lancet. Diabetes & Endocrinology; Scheen AJ, Lefèbvre PJ

Dec 26th, 2022 - 2022 corresponds to the 100th anniversary of the discovery of glucagon. This TimeCapsule aims to recall the main steps leading to the discovery, characterisation, and clinical importance of the so-called second pancreatic hormone. We describe the early historical findings in basic research (ie, discovery, purification, structure, α-cell origin, radioimmunoassay, glucagon gene [GCG], and glucago...

Glucagon-Like Peptide-1 Receptor Agonists and Dual Glucose-Dependent Insulinotropic Pol...
https://doi.org/10.1177/10742484221146371
Journal of Cardiovascular Pharmacology and Therapeutics; Muzurović EM, Volčanšek Š et. al.

Dec 23rd, 2022 - The obesity pandemic is accompanied by increased risk of developing metabolic syndrome (MetS) and related conditions: non-alcoholic fatty liver disease (NAFLD)/non-alcoholic steatohepatitis (NASH), type 2 diabetes mellitus (T2DM) and cardiovascular (CV) disease (CVD). Lifestyle, as well as an imbalance of energy intake/expenditure, genetic predisposition, and epigenetics could lead to a dysmeta...

Utilizing type 2 diabetes medications outside glycemic parameters - where are we headed?
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9870453
Current Opinion in Endocrinology, Diabetes, and Obesity; Malkani NP, Aroda VR

Dec 22nd, 2022 - Glucose-lowering medications have become strong choices for purposes beyond glucose control in both patients with and without type 2 diabetes. Recent studies have explored the use of specific glucose-lowering therapies in areas such as cardiovascular disease, renal disease, obesity, nonalcoholic fatty liver disease (NAFLD), and Alzheimer's disease, among others. This begs the question if glycem...

Alkaloids and Coumarins with Adiponectin-Secretion-Promoting Activities from the Leaves...
https://doi.org/10.1021/acs.jnatprod.2c00844
Journal of Natural Products; Nhoek P, Ahn S et. al.

Dec 20th, 2022 - Fractionation of a methanol extract of Orixa japonica leaves led to the identification of five new quinoline alkaloids (1, 2, 4, 8, and 9), three new coumarins (15, 17, and 19), and 20 known compounds. The structures were determined by analysis of 1D and 2D NMR spectroscopic data. The absolute configuration of 19 was proposed by electronic circular dichroism calculation. Among the compounds tes...

Amentoflavone Exerts Anti-Neuroinflammatory Effects by Inhibiting TLR4/MyD88/NF-κB and ...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9747320
Mediators of Inflammation; Rong S, Yang C et. al.

Dec 17th, 2022 - Amentoflavone, a natural biflavone, exerts anti-inflammation, antioxidation, and antiapoptosis effects on many diseases. However, the mechanism of amentoflavone on neuroinflammation-related diseases has not been comprehensively examined clearly. BV2 microglial cells were treated with amentoflavone (10 μM), followed by lipopolysaccharide (LPS). Microglial activation and migration ability and the...