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Role of cysteine 341 and arginine 348 of GLP-1 receptor in G-protein coupling.
cryo-electron microscopy structure of the peptide-activated GLP-1R-Gs complex at near atomic resolution
this study, we investigated whether glucagon (show GCG Proteins) and glucagon-like peptide-1 (GLP-1 (show GCG Proteins)), hormones produced by alpha cells, contribute to insulin (show INS Proteins) secretion in INS-1 (show FOXM1 Proteins) cells, a beta (show SUCLA2 Proteins) cell line. Co-treatment with glucagon (show GCG Proteins) and exendin-4 (Ex-4), a GLP-1 receptor agonist, additively increased glucose-stimulated insulin (show INS Proteins) secretion in INS-1 (show FOXM1 Proteins) cells
genetic association studies in population in Republic of Korea: Data suggest that SNPs in PAX4 (show PAX4 Proteins) and GLP1R are associated with type 2 diabetes (T2D) in the population studied. In genome-wide associations, PAX4 (show PAX4 Proteins) Arg192His increased risk of T2D; GLP1R Arg131Gln decreased risk of T2D. (PAX4 (show PAX4 Proteins) = paired box 4 (show PAX4 Proteins) protein; GLP1R = glucagon-like peptide 1 receptor)
LINC01121 functions as a tumor promoter by means of its involvement in the process of translational repression of the GLP1R and inhibition of the cAMP/PKA signaling pathway.
cryo-EM structure of the human GLP-1 receptor in complex with the G protein-biased peptide exendin-P5 and a Galphas (show GNAS Proteins) heterotrimer, determined at a global resolution of 3.3 A
The results demonstrate the exendin-4 induces a partial reduction in triglycerides in steatotic hepatocytes within 12 h via the GLP-1 receptor-mediated activation of protein kinase A. Thus, the reduction in hepatocyte triglyceride accumulation is likely driven primarily by downregulation of lipogenesis and upregulation of beta-oxidation of free fatty acids
Data (including data from studies in knockout mice) suggest that MIR204 (which is highly enriched in beta-cells) directly targets 3'-untranslated region of GLP1R and thereby down-regulates expression of GLP1R in beta-cells. Studies were also conducted in primary human and mouse beta-cells and in rat insulinoma (show RPS15 Proteins) cell line.
Data suggest that GLP1R signaling in pancreatic beta-cells leading to insulin (show INS Proteins) secretion involves interactions of GLP1R with HIP1 (show HIP1 Proteins), SNX1 (show SNX1 Proteins), and SNX27 (show SNX27 Proteins); HIP1 (show HIP1 Proteins) appears to regulate coupling of cell surface GLP1R activation with endocytosis; SNX1 (show SNX1 Proteins) and SNX27 (show SNX27 Proteins) appear to control balance between GLP1R plasma membrane recycling and lysosomal degradation.
The GLP-1R was abundantly expressed in numerous regions, including the septal nucleus, hypothalamus, and brain stem.
This is the first time that human Epicardial adipose tissue is found to express both GLP-1R and GLP-2R (show GLP2R Proteins) genes.
Changes in GLP-1 (show GCG Proteins) levels are associated with weight loss in newly diagnosed Chinese diabetes patients receiving acarbose
Presynaptic GLP-1 (show GCG Proteins) receptors enhance the depolarization-evoked release of glutamate (show GRIN1 Proteins) and GABA in the mouse cortex and hippocampus.
This study presents an unexpected proinflammatory switch from Galphas (show GNAS Proteins) to GalphaI glp1r signaling in burn monocytes which promotes ERK1/2 and NF-kappaB (show NFKB1 Proteins) activation
Glucagon (show GCG Proteins)-like peptide (GLP)-1 (show GCG Proteins) modulates epithelial ion transport indirectly by activating calcitonin gene-related peptide (CGRP (show CALCA Proteins))-containing submucosal enteric neurons in the mouse colon. This GLP-1 (show GCG Proteins)-CGRP (show CALCA Proteins) response was area-specific and could potentially contribute to the diarrheal side effect of certain GLP-1 receptor therapeutics.
Data (including data from studies using transgenic and knockout mice) suggest that Glp1 (show GCG Proteins)/Glp1r signaling in insulin (show INS Proteins)-secreting cells plays important role in development of glucose intolerance in obesity; however, Glp1r is not required in insulin (show INS Proteins)-secreting cells for improvement in glucose intolerance after weight loss due to bariatric surgery (here, vertical sleeve gastrectomy).
GLP-1R signaling in paraventricular thalamic nucleus plays a role in food intake control.
GLP-1 receptor agonists suppress the progression of atherosclerosis by inhibiting vascular smooth muscle cell proliferation and enhancing AMP-activated protein kinase (show PRKAA2 Proteins) and cell cycle regulation in ApoE (show APOE Proteins) deficient mice.
IL-33 (show IL33 Proteins), GLP-1R, and CCL20 (show CCL20 Proteins) are deregulated in human inflammatory bowel disease. GLP-1 receptor agonists upregulate IL-33 (show IL33 Proteins), mucin 5b, and CCL20 (show CCL20 Proteins) in murine Brunner's glands. GLP-1 receptor agonists affect gut (show GUSB Proteins) homeostasis in both proximal and distal parts of the gut (show GUSB Proteins).
findings identify a group of proteins that interact with GLP-1R and show that one specific interacting protein, SERP1, has an important role in facilitating the glycosylation of GLP-1R and rescuing its activities after ER stress induced by tunicamycin.
Suggest transcription factor 7-like 2 (show TCF7L2 Proteins) is a possible regulator of glucagon-like peptide 1 receptor expression in endothelial/smooth muscle cells in diabetic mice.
ventromedial hypothalamus GLP-1R regulates food intake by engaging key nutrient sensors but is dispensable for the effects of GLP-1RA on nutrient homeostasis
induces insulin secretion\; mediates neuroendocrine signaling of feeding behavior\; mediates cardiovascular response and increased blood pressure
glucagon-like peptide 1 receptor
, glucagon-like peptide 1 receptor-like
, GLP-1 receptor
, pancreatic beta cell receptor for the gluco-incretin hormone glucagon-like peptide 1