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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
Data show that exendin-4 (Ex-4) could attenuate breast cancer cell proliferation via activation of glucagonlike peptide-1 (GLP-1) receptor (GLP-1R) and subsequent inhibition of nuclear factor kappaB (NF-kappaB (show NFKB1 Proteins) ) activation.
we saw that GLP-1 (show GCG Proteins) induces phosphorylation of the epidermal growth factor receptor (show EGFR Proteins) and activation of Foxo1 (show FOXO1 Proteins), resulting in cell growth with concomitant enzyme release. Our work uncovers GLP-1 (show GCG Proteins)-induced signaling pathways in the exocrine pancreas and suggests that increases in amylase (show AMY Proteins) and lipase (show LIPG Proteins) levels in subjects treated with GLP-1 receptor agonists reflect adaptive growth rather than early-stage pancreatitis.
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.
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
GLP-1R is highly expressed within the lateral septum.
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.
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