Discovery of Palindrome Dual PPARγ‐GPR40 Agonists for Treating Type 2 Diabetes
Sign Up to like & getrecommendations! Published in 2024 at "ChemMedChem"
DOI: 10.1002/cmdc.202400492
Abstract: This work describes a first attempt of palindromic design for dual compounds that act simultaneously on peroxisome proliferator‐activated receptor gamma (PPARγ) and G‐protein‐coupled receptor 40 (GPR40) for the treatment of type 2 diabetes. The compounds were… read more here.
Keywords: discovery palindrome; gpr40; type diabetes; ppar gpr40 ... See more keywords
Oleic acid promotes prostate cancer malignant phenotype via the G protein‐coupled receptor FFA1/GPR40
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Cellular Physiology"
DOI: 10.1002/jcp.26572
Abstract: Prostate cancer (PCa) is the most commonly diagnosed malignancy in men and the second leading cause of cancer‐related death in industrialized countries. Epidemiologic evidence suggests that obesity promotes aggressive PCa. Recently, a family of Free… read more here.
Keywords: gpr40; pca; ffa1 gpr40; prostate cancer ... See more keywords
Trans-11 vaccenic acid improves glucose homeostasis in a model of type 2 diabetes by promoting insulin secretion via GPR40
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Functional Foods"
DOI: 10.1016/j.jff.2019.06.012
Abstract: Abstract It is largely unknown whether and how trans-11 vaccenic acid (VA), a ruminant trans-fatty acid with health benefits, influences glucose homeostasis in type 2 diabetes (T2D). VA was provided in diet to rats and… read more here.
Keywords: vaccenic acid; secretion; trans vaccenic; gpr40 ... See more keywords
Docosahexaenoic acid modulates brain-derived neurotrophic factor via GPR40 in the brain and alleviates diabesity-associated learning and memory deficits in mice
Sign Up to like & getrecommendations! Published in 2018 at "Neurobiology of Disease"
DOI: 10.1016/j.nbd.2018.07.002
Abstract: GPR40 (Free fatty acid receptor 1) has emerged as an important therapeutic target for diabetes. Several studies have demonstrated the association of comorbid psychiatric conditions with decreased n-3 polyunsaturated fatty acids, which may act as… read more here.
Keywords: gpr40; brain derived; diabesity; gpr40 brain ... See more keywords
Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b00982
Abstract: G protein-coupled receptor 40 (GPR40) has become an attractive target for the treatment of diabetes since it was shown clinically to promote glucose-stimulated insulin secretion. Herein, we report our efforts to develop highly selective and… read more here.
Keywords: gpr40; orally bioavailable; potent orally; discovery potent ... See more keywords
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
Sign Up to like & getrecommendations! Published in 2018 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.8b00213
Abstract: GPR40 (FFA1) is a G-protein-coupled receptor, primarily expressed in pancreatic islets and enteroendocrine L-cells, and, when activated, elicits increased insulin secretion only in the presence of elevated glucose levels. We recently reported the discovery of… read more here.
Keywords: gpr40; discovery 6226; full agonist; gpr40 full ... See more keywords
Overexpression of G protein-coupled receptor 40 protects obesity-induced cardiomyopathy through the SIRT1/LKB1/AMPK pathway.
Sign Up to like & getrecommendations! Published in 2022 at "Human gene therapy"
DOI: 10.1089/hum.2021.176
Abstract: Obesity has become a serious global public health problem, and cardiomyopathy caused by obesity has been paid more and more attention in recent years. As an important protein involved in glucose and lipid metabolism, G… read more here.
Keywords: obesity induced; ampk pathway; overexpression; gpr40 ... See more keywords
GPR40 deficiency worsens metabolic syndrome-associated periodontitis in mice.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of periodontal research"
DOI: 10.1111/jre.13107
Abstract: BACKGROUND AND OBJECTIVE G protein-coupled receptor 40 (GPR40) is a receptor for medium- and long-chain free fatty acids (FFAs). GPR40 activation improves type 2 diabetes mellitus (T2DM), metabolic syndrome (MetS), and the complications of T2DM… read more here.
Keywords: gpr40 deficiency; mets periodontitis; gpr40; mice ... See more keywords
In Silico Exploration of Ayurvedic Extract for Targeting Diabetes Mellitus and Non-alcoholic Fatty Liver Disease Via GPR120 and GPR40.
Sign Up to like & getrecommendations! Published in 2025 at "Current diabetes reviews"
DOI: 10.2174/0115733998380420250411073427
Abstract: INTRODUCTION Type 2 Diabetes Mellitus (T2DM) is the most prevalent form of hyperglycemia, often coexisting with Non-Alcoholic Fatty Liver Disease (NAFLD), as both share disrupted glucose and lipid metabolic pathways. The study aimed to explore… read more here.
Keywords: diabetes mellitus; pharmacology; gpr40; gpr120 ... See more keywords
Combiphore (Structure and Ligand based Pharmacophore) Approach for Design of GPR40 Modulators in Management of Diabetes.
Sign Up to like & getrecommendations! Published in 2018 at "Current drug discovery technologies"
DOI: 10.2174/1570163815666181008165822
Abstract: Pharmacophore mapping and molecular docking can be synergistically integrated to improve the drug design and discovery process. A rational strategy, combiphore approach, derived from the combined study of Structure and Ligand based pharmacophore has been… read more here.
Keywords: gpr40; ligand based; based pharmacophore; structure ligand ... See more keywords
GPR40 Activation Abolishes Diabetes-Induced Painful Neuropathy by Suppressing VEGF-A Expression.
Sign Up to like & getrecommendations! Published in 2022 at "Diabetes"
DOI: 10.2337/db21-0711
Abstract: G-protein coupled receptor 40 (GPR40) is a promising target to support glucose-induced insulin release in patients with diabetes type 2. Here, we studied the role of GPR40 in the regulation of the blood-nerve-barrier integrity and… read more here.
Keywords: gpr40; release; diabetes induced; vegf expression ... See more keywords