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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
crystal structure of the full-length GLP-1 receptor bound to a truncated peptide agonist
crystal structures of the human GLP-1R transmembrane domain in complex with two different negative allosteric modulators, PF-06372222 and NNC0640, at 2.7 and 3.0 A resolution, respectively
Data suggest that pancreatic level of GLP1R is highest in insulin (show INS Proteins)-secreting cells; here, highest intensity of GLP1R immunostaining was observed in beta-cells in pancreatic tissues obtained from organ-donor cadavers with type 2 diabetes.
Data show that purified glucagon-like peptide-1 (GLP-1 (show GCG Proteins)) receptor (GLP1R)GLP1R in nanodiscs that could bind to GLP-1 (show GCG Proteins) and exendin-4 and activate Gs protein.
Dapagliflozin, when added in real life to patients with T2DM treated with GLP1-R agonists, induced a further significant, albeit modest improvement in A1C and a further weight loss.
analysis of the biological binding site of exendin-4 peptide in the N-terminal domain of the intact human glucagon-like peptide-1 receptor
GLP1-R may represent a novel target for treating bronchial hyperresponsiveness.
Our studies show that GLP-1R is widely expressed throughout the human hypothalamus. The decreased expression of GLP-1R in the PVN and IFN of T2DM patients may be related to the dysregulation of feeding behavior and glucose homeostasis in type 2 diabetes mellitus.
The effects of GLP-1 (show GCG Proteins)-based therapies on blood glucose in type 2 diabetics are not mediated through microvascular responses.
In conclusion, exenatide significantly improves coronary endothelial function in patients with newly diagnosed type 2 diabetes. The effect may be mediated through activation of AMPK (show PRKAA1 Proteins)/PI3K (show PIK3CA Proteins)-Akt (show AKT1 Proteins)/eNOS (show NOS3 Proteins) pathway via a GLP-1R/cAMP-dependent mechanism.
Study showe that GLP-producing fibers interact with hypothalamic arcuate nucleus (ARC (show NOL3 Proteins)) Kiss1 (show KISS1 Proteins) cells that express GLP-1R, and GLP-1R signaling directly activates ARC (show NOL3 Proteins) Kiss1 (show KISS1 Proteins) function in an estradiol-independent manner. Pharmacological activation of GLP-1R signaling during fasting or pharmacological inhibition of CNS GLP-1R signaling during normal feeding does not alter circulating luteinizing hormone levels.
The increased calcium response mediated by secretin (show SECR Proteins) in the absence of GLP-1R was paralleled by an increased glucose-dependent insulin (show INS Proteins) response, indicating that the heterodimeric receptor complexes modulate secretin (show SECR Proteins) responses.
Menin and PRMT5 (show PRMT5 Proteins) suppress GLP1R transcript levels and PKA-mediated phosphorylation of FOXO1 (show FOXO1 Proteins) and CREB (show CREB1 Proteins).
Glp1r knockdown reduced anxiety-like behavior, implicating paraventricular nucleus GLP-1 (show GCG Proteins) signaling in behavioral stress reactivity
Enhanced beta-cell GLP-1R signaling contributes to improved glucose regulation after vertical sleeve gastrectomy by promoting increased glucose-stimulated insulin (show INS Proteins) secretion.
Results suggest a detectable but only modest role for GLP-1R signaling in mediating the effects of Roux-en-Y gastric bypass and that this role is limited to its well-described action on glucose regulation.
Hypothalamic Glp1r is sufficient but not necessary for regulation of energy balance and glucose homeostasis.
Genetic deletion of both GLP-1 (show GCG Proteins) and GIP (show GIP Proteins) receptors reveals that they are required to maintain an adequate islet number in adulthood and to maintain normal beta cell responses to glucose.
present study provides critical insights regarding the nature by which GLP-1 (show GCG Proteins) signaling controls reinforced behaviors and underscores the importance of both peripheral and central GLP-1R signaling for the regulation of addictive disorders.
CB1 (show CNR1 Proteins) activation negatively impacts GLP-1R-mediated insulin (show INS Proteins) secretion.
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