GLP-1R
Can Semaglutide Bind Tighter to GLP-1R?
... human GLP-1, semaglutide is a glucagon-like peptide-1 receptor (GLP-1R) agonist, which binds directly to GLP-1R, causing various beneficial downstream effects that reduce blood ...to ...
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Glucagon-like peptide-1 receptor (GLP-1R) signaling ameliorates dysfunctional immunity in COPD patients
... Park Memorial Institute (RPMI)-1640 complete medium containing 10% FBS, 100 U/mL penicillin, and 100 mg/mL streptomycin and then cultured with or without LIR (Victoza, Novo Nordisk, Denmark) at concentrations of 100 nM ...
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9-17-2013 12:00 AM The Synthesis and Evaluation of Peptide-Based Probes for the Imaging of RHAMM Expressing Carcinoma and GLP-1R on Pancreatic Beta Cells
... The Synthesis and Evaluation of Peptide-Based Probes for the The Synthesis and Evaluation of Peptide-Based Probes for the Imaging of RHAMM Expressing Carcinoma and GLP-1R on Imaging o[r] ...
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Advances in GLP-1 receptor targeting radiolabeled agent development and prospective of theranostics
... targeting GLP-1R has been demonstrated in diabetes with medicinal products used to stimulate insulin release, and in cancer for diagnostic imaging of ...targeting GLP-1R in the context of ...
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A mechanism for agonist activation of the glucagon-like peptide-1 (GLP-1) receptor through modelling & molecular dynamics
... (84%; GLP-1 residues will be identified with subscript * ...in GLP-1 recognition (reviewed in ...of GLP-1R. GLP-1 potency is sensitive to Arg-190 substitution, as is a synthetic variant ...
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PET/MRI enables simultaneous in vivo quantification of β-cell mass and function
... The GLP-1R has been shown to be a promising target for the quantification of β-cell mass using nuclear imaging techniques and was investigated as highly promising candidate to monitor the progressive loss ...
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Glucagon-like peptide-1 enhances cardiac L-type Ca2+ currents via activation of the cAMP-dependent protein kinase A pathway
... the GLP-1R and then the cAMP-dependent PKA ...that GLP-1 administration can reduce ischemia-reperfusion injury in part via activation of PKA, as well as via activation of other pro-survival kinases, ...
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Radiosynthesis and evaluation of an 18F–labeled silicon containing exendin-4 peptide as a PET probe for imaging insulinoma
... In this study, we evaluated an exendin-4 analogue, modified with a silicon containing building block, in order to elucidate its potential as an imaging agent for targeting GLP-1R positive insulinoma. We and ...
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CNS targeting pharmacological interventions for the metabolic syndrome
... Native GLP-1 has a half-life of 2–3 minutes due to rapid deg- radation by dipeptidyl peptidase-4 (DPP-4), and several GLP-1R agonists have been developed to provide prolonged bioavailabil- ...
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Activation of GLP-1 Receptor Enhances Neuronal Base Excision Repair via PI3K-AKT-Induced Expression of Apurinic/Apyrimidinic Endonuclease 1
... that GLP-1[32,44], EX-4 [45-47], and other agonists of GLP-1R [40,48] have a neuroprotective role against neurodegenerative cell death, traumatic brain injury, and ischemic ...of GLP-1 and ...
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Comparison of desferrioxamine and NODAGA for the gallium-68 labeling of exendin-4
... Introduction: Radiolabeled exendin-4 (Ex4) derivatives are used to target the glucagon-like peptide-1 receptor (GLP-1R) for the clinical diagnosis of insulinomas, a rare type of neuroendocrine tumor. ...
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The GIP receptor displays higher basal activity than the GLP-1 receptor but does not recruit GRK2 or arrestin3 effectively.
... human GLP-1R and GIPR subcloned into ...USA). GLP-1R and GIPR were subsequently re-ligated into ...YFP-labelled GLP-1R and GIPR (GLP- 1-YFP and GIPR-YFP) were purchased ...
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Effect of hCMSCs and liraglutide combination in ALI through cAMP/PKAc/β-catenin signaling pathway
... UK), GLP-1R (Novus, NBP1-97308SS, USA), p-β-catenin (Santa cruz, sc-57535, USA), TCF7L2 (Abways, CY5720, China), SFTPC (Abclonal, A11764, USA), β-catenin (Abways, CY3523, China), FGF10 (Abclo- nal, A1201, ...
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The GLP-1 agonist, liraglutide, ameliorates inflammation through the activation of the PKA/CREB pathway in a rat model of knee osteoarthritis
... via GLP-1R binding and induction [9]. GLP-1 not only regulates blood glucose levels, but is also closely associated with various pathophysiological processes, such as ...Thus, GLP-1R ...
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Liraglutide dictates macrophage phenotype in apolipoprotein E null mice during early atherosclerosis
... with GLP-1R agonists have now been established, investigating the effects of GLP-1R agonists on athero- sclerosis-associated inflammation and determining their atheroprotective mechanism is ...
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A comparison of three 67/68Ga-labelled exendin-4 derivatives for β-cell imaging on the GLP-1 receptor: the influence of the conjugation site of NODAGA as chelator
... Background: Various diseases derive from pathologically altered β -cells. Their function can be increased, leading to hyperinsulinism, or decreased, resulting in diabetes. Non-invasive imaging of the β -cell-specific ...
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Exenatide infusion decreases atrial natriuretic peptide levels by reducing cardiac filling pressures in type 2 diabetes patients with decompensated congestive heart failure
... a GLP-1R–ANP axis has been suggested in rodents [12], we aimed to investigate whether such an associa- tion between GLP-1R mediated hemodynamic effects and plasma ANP changes in patients with ...
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64Cu Labeled Sarcophagine Exendin-4 for MicroPET Imaging of Glucagon like Peptide-1 Receptor Expression
... native GLP-1 is degraded rapidly by dipeptidyl peptidase-IV (DPP-IV), several studies have conjugated different chelators to a more stable analog of GLP-1 (such as exendin-4) as PET or SPECT imaging agents ...
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Glucagon like peptide 1 receptors in the brain: controlling food intake and body weight
... link GLP-1R signaling to body weight reg- ulation in different species is challenging due to the complexity of pathways that regulate food intake and energy expendi- ...that GLP-1 inhibits food ...
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Do incretins improve endothelial function?
... identified: GLP-1, derived from the L-cells of the distal small intestine and large bowel, and glucose-dependent insulinotropic polypeptide (GIP), de- rived from the K-cells of the proximal small ...intestine. ...
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