From GLP1 receptor agonists to triple hormone receptor activation supplemented with glucagon receptor agonism.
Orv Hetil. 2023 Oct 22;164(42):1656-1664. doi: 10.1556/650.2023.32894. Print 2023 Oct 22.ABSTRACTFollowing the introduction of mono- and then dual hormone (incretin) receptor agonists into therapy, attention was turned to multiple receptor stimulation, with the additional activation of the glucagon receptor, as a new option for the pharmaceutical treatment of type 2 diabetes and obesity. In addition to its role in carbohydrate metabolism, the article reviews the other important physiological tasks of glucagon, especially its participation in intrainsular paracrine regulation, energy expenditure and the shaping of appetite ...
Source: Orvosi Hetilap - October 22, 2023 Category: General Medicine Authors: G ábor Winkler J ános Tibor Kis Krisztina Arapovicsn é Kiss L ászló Schandl Source Type: research
From GLP1 receptor agonists to triple hormone receptor activation supplemented with glucagon receptor agonism.
Orv Hetil. 2023 Oct 22;164(42):1656-1664. doi: 10.1556/650.2023.32894. Print 2023 Oct 22.ABSTRACTFollowing the introduction of mono- and then dual hormone (incretin) receptor agonists into therapy, attention was turned to multiple receptor stimulation, with the additional activation of the glucagon receptor, as a new option for the pharmaceutical treatment of type 2 diabetes and obesity. In addition to its role in carbohydrate metabolism, the article reviews the other important physiological tasks of glucagon, especially its participation in intrainsular paracrine regulation, energy expenditure and the shaping of appetite ...
Source: Orvosi Hetilap - October 22, 2023 Category: General Medicine Authors: G ábor Winkler J ános Tibor Kis Krisztina Arapovicsn é Kiss L ászló Schandl Source Type: research
From GLP1 receptor agonists to triple hormone receptor activation supplemented with glucagon receptor agonism.
Orv Hetil. 2023 Oct 22;164(42):1656-1664. doi: 10.1556/650.2023.32894. Print 2023 Oct 22.ABSTRACTFollowing the introduction of mono- and then dual hormone (incretin) receptor agonists into therapy, attention was turned to multiple receptor stimulation, with the additional activation of the glucagon receptor, as a new option for the pharmaceutical treatment of type 2 diabetes and obesity. In addition to its role in carbohydrate metabolism, the article reviews the other important physiological tasks of glucagon, especially its participation in intrainsular paracrine regulation, energy expenditure and the shaping of appetite ...
Source: Orvosi Hetilap - October 22, 2023 Category: General Medicine Authors: G ábor Winkler J ános Tibor Kis Krisztina Arapovicsn é Kiss L ászló Schandl Source Type: research
Differential effect of gastric bypass versus sleeve gastrectomy on insulinotropic action of endogenous incretins
CONCLUSIONS: After GB, increasing incretin activity augments prandial β-cell response whereas the β-cell sensitivity to increasing plasma concentrations of endogenous incretin is diminished.PMID:37853989 | DOI:10.1002/oby.23872 (Source: Obesity)
Source: Obesity - October 19, 2023 Category: Eating Disorders & Weight Management Authors: Marzieh Salehi Richard Peterson Devjit Tripathy Samantha Pezzica Ralph DeFronzo Amalia Gastaldelli Source Type: research
Differential effect of gastric bypass versus sleeve gastrectomy on insulinotropic action of endogenous incretins
CONCLUSIONS: After GB, increasing incretin activity augments prandial β-cell response whereas the β-cell sensitivity to increasing plasma concentrations of endogenous incretin is diminished.PMID:37853989 | DOI:10.1002/oby.23872 (Source: Obesity)
Source: Obesity - October 19, 2023 Category: Eating Disorders & Weight Management Authors: Marzieh Salehi Richard Peterson Devjit Tripathy Samantha Pezzica Ralph DeFronzo Amalia Gastaldelli Source Type: research
A specific gut microbiota signature is associated with an enhanced GLP-1 and GLP-2 secretion and improved metabolic control in patients with type 2 diabetes after metabolic Roux-en-Y gastric bypass
ConclusionsPatients with obesity and T2D submitted to mRYGB show an enhanced incretin response, a reduced gut permeability and a metabolic improvement, associated with a specific microbiota signature. (Source: Frontiers in Endocrinology)
Source: Frontiers in Endocrinology - October 17, 2023 Category: Endocrinology Source Type: research
Novel cannabinoid receptor 1 inverse agonist CRB-913 enhances efficacy of tirzepatide, semaglutide, and liraglutidein the diet-induced obesity mouse model
CONCLUSIONS: CRB-913 in combination with incretin analogues could deliver meaningful improvements over current standards of care for obesity and related conditions.PMID:37840407 | DOI:10.1002/oby.23902 (Source: Obesity)
Source: Obesity - October 16, 2023 Category: Eating Disorders & Weight Management Authors: Marshall Morningstar Andrew Kolodziej Suzie Ferreira Tracy Blumen Rachael Brake Yuval Cohen Source Type: research
Novel cannabinoid receptor 1 inverse agonist CRB-913 enhances efficacy of tirzepatide, semaglutide, and liraglutidein the diet-induced obesity mouse model
CONCLUSIONS: CRB-913 in combination with incretin analogues could deliver meaningful improvements over current standards of care for obesity and related conditions.PMID:37840407 | DOI:10.1002/oby.23902 (Source: Obesity)
Source: Obesity - October 16, 2023 Category: Eating Disorders & Weight Management Authors: Marshall Morningstar Andrew Kolodziej Suzie Ferreira Tracy Blumen Rachael Brake Yuval Cohen Source Type: research
Treatment with the dual-incretin agonist DA-CH5 demonstrates potent therapeutic effect in a rat model of Wolfram Syndrome
ConclusionWe present preclinical evidence for the pleiotropic therapeutic effects of long-term dual incretin agonist treatment; effects were seen despite treatment beginning after symptom-onset, indicating reversal of disease progression. Dual incretins represent a promising therapeutic avenue for WS patients. (Source: Frontiers in Endocrinology)
Source: Frontiers in Endocrinology - October 13, 2023 Category: Endocrinology Source Type: research
Pharmacological modulation of adaptive thermogenesis: new clues for obesity management?
AbstractBackgroundAdaptive
thermogenesis represents the main mechanism through which the body generates heat in response to external stimuli, a phenomenon that includes shivering and non-shivering thermogenesis. The non-shivering thermogenesis is mainly exploited by adipose tissue characterized by a brown aspect, which specializes in energy dissipation. A decreased amount of brown adipose tissue has been observed in ageing and chronic illnesses such as obesity, a worldwide health problem characterized by dysfunctional adipose tissue expansion and associated cardiometabolic complications. In the last decades, the discov...
Source: Journal of Endocrinological Investigation - October 7, 2023 Category: Endocrinology Source Type: research
How should we think about the unprecedented weight loss efficacy of incretin-mimetic drugs?
(Source: Journal of Clinical Investigation)
Source: Journal of Clinical Investigation - October 3, 2023 Category: Biomedical Science Authors: Yang Gou, Michael W. Schwartz Source Type: research
Surfactant-like photosensitizer for endoscopic duodenal ablation: Modulating meal-stimulated incretin hormones in obese and type 2 diabetes
Biomaterials. 2023 Sep 23;302:122336. doi: 10.1016/j.biomaterials.2023.122336. Online ahead of print.ABSTRACTDuodenal ablation improves glycaemic control and weight loss, so it has been applied using hydrothermal catheters in obese and type 2 diabetes patients, indicating similar mechanisms and therapeutic effects as bariatric surgeries. Endoscopic photodynamic therapy is an innovative procedure that easily accessible to endocrine or gastrointestinal organs, so it is critical for the sprayed photosensitizer (PS) to long-term interact with target tissues for enhancing its effects. Surfactant-like PS was more stable in a wid...
Source: Biomaterials - October 1, 2023 Category: Materials Science Authors: Sanghee Lee Moon Jae Chung Minji Ahn Hyun Jin Park Eun Kyung Wang Taeeun Guon Hyun Jung Kee Cheol Ryong Ku Kun Na Source Type: research
Surfactant-like photosensitizer for endoscopic duodenal ablation: Modulating meal-stimulated incretin hormones in obese and type 2 diabetes
Biomaterials. 2023 Sep 23;302:122336. doi: 10.1016/j.biomaterials.2023.122336. Online ahead of print.ABSTRACTDuodenal ablation improves glycaemic control and weight loss, so it has been applied using hydrothermal catheters in obese and type 2 diabetes patients, indicating similar mechanisms and therapeutic effects as bariatric surgeries. Endoscopic photodynamic therapy is an innovative procedure that easily accessible to endocrine or gastrointestinal organs, so it is critical for the sprayed photosensitizer (PS) to long-term interact with target tissues for enhancing its effects. Surfactant-like PS was more stable in a wid...
Source: Biomaterials - October 1, 2023 Category: Materials Science Authors: Sanghee Lee Moon Jae Chung Minji Ahn Hyun Jin Park Eun Kyung Wang Taeeun Guon Hyun Jung Kee Cheol Ryong Ku Kun Na Source Type: research
Mechanisms of action of incretin receptor based dual- and tri-agonists in pancreatic islets
Am J Physiol Endocrinol Metab. 2023 Sep 20. doi: 10.1152/ajpendo.00236.2023. Online ahead of print.ABSTRACTSimultaneous activation of the incretin G protein coupled receptors via unimolecular dual-receptor agonists (UDRA) has emerged as a new therapeutic approach for type 2 diabetes. Recent studies also advocate triple agonism with molecules also capable of binding the glucagon receptor. In this scoping review we discuss the cellular mechanisms of action (MOA) underlying the actions of these novel and therapeutically important classes of peptide receptor agonists. Clinical efficacy studies of several UDRAs have demonstrate...
Source: American Journal of Physiology. Endocrinology and Metabolism - September 20, 2023 Category: Physiology Authors: Franco Folli Giovanna Finzi Roberto Manfrini Alessandra Galli Francesca Casiraghi Lucia Centofanti Cesare Berra Paolo Fiorina Alberto Davalli Stefano La Rosa Carla Perego Paul B Higgins Source Type: research
Endoplasmic Reticulum Stress in Pancreatic β-Cells Induces Incretin Desensitization and β-Cell Dysfunction via ATF4-Mediated PDE4D Expression
Am J Physiol Endocrinol Metab. 2023 Sep 20. doi: 10.1152/ajpendo.00156.2023. Online ahead of print.ABSTRACTPancreatic β-cell dysfunction and eventual loss are key steps in the progression of type 2 diabetes (T2D). Endoplasmic reticulum (ER) stress responses, especially those mediated by the PERK-ATF4 pathway, have been implicated in promoting these β-cell pathologies. However, the exact molecular events surrounding the role of the PERK-ATF4 pathway in β-cell dysfunction remain unknown. Here, we report our discovery that ATF4 promotes the expression of PDE4D, which disrupts β-cell function via a downregulation of cAMP s...
Source: American Journal of Physiology. Endocrinology and Metabolism - September 20, 2023 Category: Physiology Authors: Ji-Hye Lee Hanguk Ryu Hyejin Lee Hye Ram Yu Yurong Gao Kyeong-Min Lee Young-Joon Kim Jaemin Lee Source Type: research
