Médecine des Maladies Métaboliques, Journal Year: 2024, Volume and Issue: unknown
Published: Nov. 1, 2024
Signal Transduction and Targeted Therapy, Journal Year: 2024, Volume and Issue: 9(1)
Published: Sept. 18, 2024
The glucagon-like peptide-1 (GLP-1) receptor, known as GLP-1R, is a vital component of the G protein-coupled receptor (GPCR) family and found primarily on surfaces various cell types within human body. This specifically interacts with GLP-1, key hormone that plays an integral role in regulating blood glucose levels, lipid metabolism, several other crucial biological functions. In recent years, GLP-1 medications have become focal point medical community due to their innovative treatment mechanisms, significant therapeutic efficacy, broad development prospects. article thoroughly traces developmental milestones drugs, from initial discovery clinical application, detailing evolution diverse along distinct pharmacological properties. Additionally, this paper explores potential applications agonists (GLP-1RAs) fields such neuroprotection, anti-infection measures, reduction inflammation, enhancement cardiovascular function. It provides in-depth assessment effectiveness GLP-1RAs across multiple body systems-including nervous, cardiovascular, musculoskeletal, digestive systems. includes integrating latest trial data delving into signaling pathways mechanisms. primary goal emphasize extensive benefits using treating spectrum diseases, obesity, non-alcoholic fatty liver disease (NAFLD), neurodegenerative musculoskeletal forms cancer. ongoing new indications for drugs offers promising prospects further expanding interventions, showcasing field.
Language: Английский
Citations
97
Peptides, Journal Year: 2025, Volume and Issue: 187, P. 171380 - 171380
Published: March 11, 2025
Recent studies with peptide-based incretin herapies have focussed mainly on the glucagon-like peptide-1 (GLP-1) receptor agonist semaglutide and dual tirzepatide that engages receptors for GLP-1 glucose-dependent insulinotropic polypeptide (GIP). Randomised clinical trials 'real-world' confirmed marked glucose-lowering weight-lowering efficacy of these agents across diverse populations. These include different ethnic groups, young elderly individuals without diabetes and/or overweight or obesity. also protections against development progression cardiovascular renal diseases are additive to benefits conferred by improved control blood glucose body weight. Emerging evidence suggests therapies could additionally ameliorate fatty liver disease, chronic inflammation, sleep apnea possibly degenerative bone disorders cognitive decline. New incretin-based peptide in a long-acting glucagon (LY3324954), GLP-1/glucagon agonists (survodutide, pemvidutide, mazdutide, G49), triple GLP-1/GIP/glucagon (retatrutide, efocipegtrutide), combination amylin analogue cagrilintide (CagriSema), unimolecular GLP-1/amylin (amycretin), GIP antibody agonism (MariTide). The creation multi-targeting synthetic peptides provides opportunities management type 2 obesity as well new therapeutic approaches an expanding list associated co-morbidities. aim review is acquaint reader developments field from 2023 present (February 2025).
Language: Английский
Citations
1
Peptides, Journal Year: 2024, Volume and Issue: 175, P. 171180 - 171180
Published: Feb. 22, 2024
Investigations conducted since 2018 have identified several host-defense peptides present in frog skin secretions whose properties suggest the possibility of their development into a new class agent for Type 2 diabetes (T2D) therapy. Studies vitro described that (a) stimulate insulin release from BRIN-BD11 clonal β-cells and isolated mouse islets, (b) display β-cell proliferative activity protect against cytokine-mediated apoptosis (c) production anti-inflammatory cytokine IL-10 inhibit pro-inflammatory cytokines TNF-α IL-1β. Rhinophrynin-27, phylloseptin-3.2TR temporin F are with therapeutic potential. vivo carried out db/db high fat-fed mice shown twice-daily administration [S4K]CPF-AM1 [A14K]PGLa-AM1, analogs first octoploid Xenopus amieti, over 28 days lowers circulating glucose HbA1c concentrations, increases sensitivity improves tolerance lipid profile. Peptide treatment produced potentially beneficial changes expression skeletal muscle genes involved signaling islet secretion these murine models T2D. Lead compounds uncovered by study HDPs may provide basis design types agents can be used, alone or combination existing therapies,
Language: Английский
Citations
5
Analytica Chimica Acta, Journal Year: 2025, Volume and Issue: 1350, P. 343853 - 343853
Published: Feb. 22, 2025
Language: Английский
Citations
0
European Journal of Pharmacology, Journal Year: 2024, Volume and Issue: 985, P. 177095 - 177095
Published: Nov. 6, 2024
Language: Английский
Citations
3
Frontiers in Pharmacology, Journal Year: 2024, Volume and Issue: 15
Published: July 8, 2024
Aims: Glucagon-like peptide-1 receptor agonists (GLP-1 RAs) are employed extensively in the management of type 2 diabetes and obesity. However, there is a paucity real-world data on their safety tolerability for metabolic nutritional adverse events large sample populations. This study aimed to analyse signatures different GLP-1 RAs by exploring Food Drug Administration (FDA) Adverse Event Reporting System (FAERS). Methods: AEs were extracted from FDA database each RA time its launch until second quarter 2023. The reported odds ratio (ROR), proportional reporting (PRR), Empirical Bayesian Geometric Mean Confidence Propagation Neural Network identify AE signals. Results: A system organ class metabolism nutrition disorders was filter reports, resulting identification 10,450 reports exenatide, 2,860 liraglutide, 240 albiglutide, 4,847 dulaglutide, 2,905 semaglutide, 1,089 tirzepatide, 13 lixisenatide. Semaglutide (ROR, 3.34; 95%CI, 3.22), liraglutide 2.78; 2.69), exenatide 2.15; 2.11) associated with disorders. number signals detected as follows: albiglutide (n = 1), lixisenatide 2), tirzepatide 11), 12), 16), semaglutide 20), dulaglutide 22). Dehydration most frequent contributing serious outcomes 318, 23.93%), 434, 20.90%), 370, 25.10%) 70, 32.86%). onset (TTO) statistically between other ( p < 0.001), Weibull parameters dehydration analyses all showed an early failure-type profile. Conclusion: Our suggests that more susceptible than RAs. Liraglutide, tirzepaptide’s potential induce dehydration, necessitates special attention. Despite certain deficiencies, have considerable treatment eating
Language: Английский
Citations
2
Retos, Journal Year: 2024, Volume and Issue: 55, P. 296 - 301
Published: March 27, 2024
Obesity is reported to be strongly associated with low levels of adiponectin, which may involved in metabolic syndrome, insulin resistance, cardiovascular disease, hypertension, and cancer cell proliferation. Meanwhile, physical exercise has been increase adiponectin decrease resistance obese individuals. Therefore, this study aimed prove the effects four weeks moderate-intensity combination (aerobic resistance) on increasing levels, skeletal muscle mass (SMM), decreasing fat (FM) women. A total 14 adolescent women aged 20-24 years a body index (BMI) 27.5-36.5 kg/m2 (based Asia-Pacific BMI classification) were selected as research subjects divided into two intervention groups: control (CON) (MCE) groups. The ELISA kit method was used analyze pre- post-exercise while mBCA 554 seca measure BMI, FM, SMM. Statistical analysis performed using an independent samples t-test 5% significance level. data showed ∆-BMI between CON MCE (0.54±0.99 vs -1.31±0.19 kg/m2; p = 0.001), ∆-FM (1.56±3.89 -3.60±1.16 kg; 0.006), ∆-SMM (-0.85±1.91 3.61±0.74 ∆-Adiponectin (0.55±2.39 15.45±6.21 ng/mL; 0.001). results demonstrate that 4-week effectively increases reduces Keywords: Obesity, exercise, composition.
Language: Английский
Citations
1
Peptides, Journal Year: 2024, Volume and Issue: 177, P. 171212 - 171212
Published: April 11, 2024
Surprisingly, agonists, as well antagonists of the glucose-dependent insulinotropic polypeptide receptor (GIPR), are currently being used or investigated treatment options for type 2 diabetes and obesity - both, when combined with glucagon-like peptide 1 (GLP-1R) agonism, enhance GLP-1-induced glycemia weight loss further. This paradox raises several questions regarding not only mechanisms actions GIP but also processes engaged during activation both GLP-1 receptors. Here, we provide an overview studies properties peptide-derived GIPR antagonists, focusing on GIP(3-30)NH
Language: Английский
Citations
1
American Journal of Therapeutics, Journal Year: 2024, Volume and Issue: 31(4), P. e523 - e527
Published: July 1, 2024
1Division of Diabetes, Endocrinology, and Metabolism, Department Medicine, Vanderbilt University Medical Center, Nashville, TN 2Gene Labs, Gaza, Palestine The authors have no conflicts interest to declare.
Language: Английский
Citations
1
Journal of Clinical Investigation, Journal Year: 2024, Volume and Issue: 134(24)
Published: Oct. 22, 2024
Following a meal, glucagon-like peptide-1 (GLP1) and glucose-dependent insulinotropic polypeptide (GIP), the two major incretins promoting insulin release, are secreted from specialized enteroendocrine cells (L- K-cells, respectively). Although GIP is dominant incretin in humans, detailed molecular mechanisms governing its release remain to be explored. secretion regulated by activity of G protein-coupled receptors (GPCRs) expressed K-cells. GPCRs couple one or more specific classes heterotrimeric proteins. In present study, we focused on potential metabolic roles K-cell Gs. First, generated mouse model that allowed us selectively stimulate Gs signaling. Second, strain harboring an inactivating mutation Gnas, gene encoding alpha-subunit Gs, Metabolic phenotyping studies showed acute chronic stimulation signaling greatly improved impaired glucose homeostasis obese mice type 2 diabetes, due enhanced secretion. contrast, K-cell-specific Gnas knockout displayed markedly reduced plasma levels. These data strongly suggest strategies aimed at enhancing may prove useful for treatment diabetes related diseases.
Language: Английский
Citations
1