Brain access of incretins and incretin receptor agonists to their central targets relevant for appetite suppression and weight loss
Am J Physiol Endocrinol Metab. 2024 Feb 21. doi: 10.1152/ajpendo.00250.2023. Online ahead of print.ABSTRACTIncretin-based pharmacotherapies provide novel efficient and safe therapeutic options to curb appetite and produce weight loss in obese patients. Delivered systemically, these molecules produce pleiotropic metabolic benefits, but the target sites mediating their weight-suppressive action are located within the brain. Recent research has increased our understanding of the neural circuits and behavioural mechanisms involved in the anorectic and metabolic consequences of glucagon-like peptide 1 (GLP-1)-based weight loss ...
Source: American Journal of Physiology. Endocrinology and Metabolism - February 21, 2024 Category: Physiology Authors: Sophie Buller Clemence Blouet Source Type: research

Brain access of incretins and incretin receptor agonists to their central targets relevant for appetite suppression and weight loss
Am J Physiol Endocrinol Metab. 2024 Feb 21. doi: 10.1152/ajpendo.00250.2023. Online ahead of print.ABSTRACTIncretin-based pharmacotherapies provide novel efficient and safe therapeutic options to curb appetite and produce weight loss in obese patients. Delivered systemically, these molecules produce pleiotropic metabolic benefits, but the target sites mediating their weight-suppressive action are located within the brain. Recent research has increased our understanding of the neural circuits and behavioural mechanisms involved in the anorectic and metabolic consequences of glucagon-like peptide 1 (GLP-1)-based weight loss ...
Source: Am J Physiol Endocri... - February 21, 2024 Category: Endocrinology Authors: Sophie Buller Clemence Blouet Source Type: research

Brain access of incretins and incretin receptor agonists to their central targets relevant for appetite suppression and weight loss
Am J Physiol Endocrinol Metab. 2024 Feb 21. doi: 10.1152/ajpendo.00250.2023. Online ahead of print.ABSTRACTIncretin-based pharmacotherapies provide novel efficient and safe therapeutic options to curb appetite and produce weight loss in obese patients. Delivered systemically, these molecules produce pleiotropic metabolic benefits, but the target sites mediating their weight-suppressive action are located within the brain. Recent research has increased our understanding of the neural circuits and behavioural mechanisms involved in the anorectic and metabolic consequences of glucagon-like peptide 1 (GLP-1)-based weight loss ...
Source: American Journal of Physiology. Endocrinology and Metabolism - February 21, 2024 Category: Physiology Authors: Sophie Buller Clemence Blouet Source Type: research

Brain access of incretins and incretin receptor agonists to their central targets relevant for appetite suppression and weight loss
Am J Physiol Endocrinol Metab. 2024 Feb 21. doi: 10.1152/ajpendo.00250.2023. Online ahead of print.ABSTRACTIncretin-based pharmacotherapies provide novel efficient and safe therapeutic options to curb appetite and produce weight loss in obese patients. Delivered systemically, these molecules produce pleiotropic metabolic benefits, but the target sites mediating their weight-suppressive action are located within the brain. Recent research has increased our understanding of the neural circuits and behavioural mechanisms involved in the anorectic and metabolic consequences of glucagon-like peptide 1 (GLP-1)-based weight loss ...
Source: Am J Physiol Endocri... - February 21, 2024 Category: Endocrinology Authors: Sophie Buller Clemence Blouet Source Type: research

Brain access of incretins and incretin receptor agonists to their central targets relevant for appetite suppression and weight loss
Am J Physiol Endocrinol Metab. 2024 Feb 21. doi: 10.1152/ajpendo.00250.2023. Online ahead of print.ABSTRACTIncretin-based pharmacotherapies provide novel efficient and safe therapeutic options to curb appetite and produce weight loss in obese patients. Delivered systemically, these molecules produce pleiotropic metabolic benefits, but the target sites mediating their weight-suppressive action are located within the brain. Recent research has increased our understanding of the neural circuits and behavioural mechanisms involved in the anorectic and metabolic consequences of glucagon-like peptide 1 (GLP-1)-based weight loss ...
Source: American Journal of Physiology. Endocrinology and Metabolism - February 21, 2024 Category: Physiology Authors: Sophie Buller Clemence Blouet Source Type: research

Brain access of incretins and incretin receptor agonists to their central targets relevant for appetite suppression and weight loss
Am J Physiol Endocrinol Metab. 2024 Feb 21. doi: 10.1152/ajpendo.00250.2023. Online ahead of print.ABSTRACTIncretin-based pharmacotherapies provide novel efficient and safe therapeutic options to curb appetite and produce weight loss in obese patients. Delivered systemically, these molecules produce pleiotropic metabolic benefits, but the target sites mediating their weight-suppressive action are located within the brain. Recent research has increased our understanding of the neural circuits and behavioural mechanisms involved in the anorectic and metabolic consequences of glucagon-like peptide 1 (GLP-1)-based weight loss ...
Source: Am J Physiol Endocri... - February 21, 2024 Category: Endocrinology Authors: Sophie Buller Clemence Blouet Source Type: research

GPR119 agonists for type 2 diabetes: past failures and future hopes for preclinical and early phase candidates
This article reviews studies focused on GPR119 agonism in animal models of T2D and in patients with T2D.EXPERT OPINION: GPR119 agonists in vitro and in vivo can potentially regulate incretin hormone release from the gut, then pancreatic insulin release which regulates blood glucose concentrations. However, the success in controlling glucose homeostasis in rodent models of T2D and obesity, failed to translate to early-stage clinical trials in patients with T2D. However, in more recent studies, acute and chronic dosing with the GPR119 agonist DS-8500a had increased efficacy, although this compound was discontinued for furthe...
Source: Expert Opinion on Investigational Drugs - February 19, 2024 Category: Drugs & Pharmacology Authors: Deanne H Hryciw Rhiannon K Patten Raymond J Rodgers Joseph Proietto Dana S Hutchinson Andrew J McAinch Source Type: research

GPR119 agonists for type 2 diabetes: past failures and future hopes for preclinical and early phase candidates
This article reviews studies focused on GPR119 agonism in animal models of T2D and in patients with T2D.EXPERT OPINION: GPR119 agonists in vitro and in vivo can potentially regulate incretin hormone release from the gut, then pancreatic insulin release which regulates blood glucose concentrations. However, the success in controlling glucose homeostasis in rodent models of T2D and obesity, failed to translate to early-stage clinical trials in patients with T2D. However, in more recent studies, acute and chronic dosing with the GPR119 agonist DS-8500a had increased efficacy, although this compound was discontinued for furthe...
Source: Expert Opinion on Investigational Drugs - February 19, 2024 Category: Drugs & Pharmacology Authors: Deanne H Hryciw Rhiannon K Patten Raymond J Rodgers Joseph Proietto Dana S Hutchinson Andrew J McAinch Source Type: research

Comparative effects of incretin-based therapy on doxorubicin-induced nephrotoxicity in rats: the role of SIRT1/Nrf2/NF- κB/TNF-α signaling pathways
This study aimed to investigate whether the two pathways of incretin-based therapy, glucagon-like peptide-1 receptor agonist (presented as semaglutide, SEM) and dipeptidyl peptidase-4 inhibitor (presented as alogliptin, ALO), differentially protect against DOX-induced nephrotoxicity in rats and to clarify the underlying molecular mechanisms.Methods: Adult male rats were divided into six groups: control (received the vehicle), DOX (20 mg/kg, single I.P. on day 8), DOX + ALO (20 mg/kg/day, P.O. for 10 days), DOX + SEM (12 μg/kg/day, S.C. for 10 days), ALO-alone, and SEM-alone groups. At the end of the study, the animal...
Source: Frontiers in Pharmacology - February 19, 2024 Category: Drugs & Pharmacology Source Type: research

The Role of G Protein-Coupled Receptors and Receptor Kinases in Pancreatic < em > β < /em > -Cell Function and Diabetes
Pharmacol Rev. 2024 Feb 13;76(2):267-299. doi: 10.1124/pharmrev.123.001015.ABSTRACTType 2 diabetes (T2D) mellitus has emerged as a major global health concern that has accelerated in recent years due to poor diet and lifestyle. Afflicted individuals have high blood glucose levels that stem from the inability of the pancreas to make enough insulin to meet demand. Although medication can help to maintain normal blood glucose levels in individuals with chronic disease, many of these medicines are outdated, have severe side effects, and often become less efficacious over time, necessitating the need for insulin therapy. G prot...
Source: Pharmacological Reviews - February 13, 2024 Category: Drugs & Pharmacology Authors: Matthew J Varney Jeffrey L Benovic Source Type: research

The Role of G Protein-Coupled Receptors and Receptor Kinases in Pancreatic < em > β < /em > -Cell Function and Diabetes
Pharmacol Rev. 2024 Feb 13;76(2):267-299. doi: 10.1124/pharmrev.123.001015.ABSTRACTType 2 diabetes (T2D) mellitus has emerged as a major global health concern that has accelerated in recent years due to poor diet and lifestyle. Afflicted individuals have high blood glucose levels that stem from the inability of the pancreas to make enough insulin to meet demand. Although medication can help to maintain normal blood glucose levels in individuals with chronic disease, many of these medicines are outdated, have severe side effects, and often become less efficacious over time, necessitating the need for insulin therapy. G prot...
Source: Pharmacological Reviews - February 13, 2024 Category: Drugs & Pharmacology Authors: Matthew J Varney Jeffrey L Benovic Source Type: research

G protein-coupled receptors driven intestinal glucagon-like peptide-1 reprogramming for obesity: Hope or hype?
Biomed Pharmacother. 2024 Feb 9;172:116245. doi: 10.1016/j.biopha.2024.116245. Online ahead of print.ABSTRACT'Globesity' is a foremost challenge to the healthcare system. The limited efficacy and adverse effects of available oral pharmacotherapies pose a significant obstacle in the fight against obesity. The biology of the leading incretin hormone glucagon-like-peptide-1 (GLP-1) has been highly captivated during the last decade owing to its multisystemic pleiotropic clinical outcomes beyond inherent glucoregulatory action. That fostered a pharmaceutical interest in synthetic GLP-1 analogues to tackle type-2 diabetes (T2D),...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - February 10, 2024 Category: Drugs & Pharmacology Authors: Mohan Patil Ilaria Casari Leon N Warne Marco Falasca Source Type: research

Isomaltulose Enhances GLP ‐1 and PYY Secretion to a Mixed Meal in People With or Without Type 2 Diabetes as Compared to Saccharose
ConclusionA snack containing ISO markedly enhances the release of the metabolically advantageous gut hormones PYY and GLP-1 and enhances GIP release in response to a subsequent complex meal. (Source: Molecular Nutrition and Food Research)
Source: Molecular Nutrition and Food Research - February 9, 2024 Category: Food Science Authors: Jiudan Zhang, Dominik Sonnenburg, Domenico Tric ò, Stefan Kabisch, Andrea Mari, Stephan Theis, Margrit Kemper, Olga Pivovarova‐Ramich, Sascha Rohn, Andreas F. H. Pfeiffer Tags: Research Article Source Type: research