Receptors Structure and subtype The receptor of GLP-1 (GLP1R) is a seventransmembrane GPCR that belongs to a subclass of the family B. The GLP-1 receptor was first identified by ligand binding experiments and measurements of cyclic AMP accumulation using the rat insulinoma cell line.3 The huma...
GLP-1 agonist medications work bymimickingthis hormone. In medication terms, anagonistis amanufacturedsubstance that attaches to a cell receptor and causes the same action as the naturally occurring substance. In other words, GLP-1 medications bind to GLP receptors to trigger the effects (or roles...
Stimulation of the cognate receptors on the taste bud cells with sweet compound results in a release of GLP-1. Higher concentrations of sweet stimuli produced higher GLP-1 stimulation [12]. The released GLP-1 activated GLP-1 R on the gustatory nerve fibres in close proximity to GLP-1-...
Both GIP and GLP-1 work by binding to different G-protein-coupled receptors (GPCRs). These receptors belong to the class B/II GPCR family, which consists of seven transmembrane GPCRs [4], [5], [6], [7]. In a glucose-dependent manner, activation of both incretin receptors on cells ...
A potential alternative treatment strategy for T2D is through the modulation of endogenous GLP-1 secretion; however, the factors and pathways involved in the regulation of endogenous GLP-1 secretion remain incompletely understood. G protein-coupled receptors (GPCRs) regulate GLP-1 secretion in EECs ...
Glucagon-like peptide-1 receptors (GLP-1Rs) are a new type of hypoglycemic drugs that enhance insulin secretion and inhibit glucagon secretion in a glucose concentration-dependent manner. Activation of GLP-1Rs can delay gastric emptying and reduce food intake through appetite suppression as they act...
Outside of these functions, GLP receptors are also expressed in the human retina and are thought to be involved in the prevention of retinal neurodegeneration, an early event in diabetic retinopathy [23]. Additionally, both GLP-1 and GIP play a role in cardiovascular disease, as agonists of ...
GLPG2938 is an orally active, potent and selective S1P2 receptor (S1PR2) antagonist (GTPγS induction IC50 = 29 nM; [S1P] = EC80) with no activity against other S1P receptors. GLPG2938 inhibits sphingosine 1-phosphate (S1P)-induced cellular responses in cultures (Ca2+ flux IC50 = 8.8 ...
The mutein exhibits reduced affinity for Fc receptors. In other embodiments, the variable portion of the heavy and/or light chains of an anti-GCGR antibody can be substituted for the variable portion of an antibody heavy and/or light chain. Alternatively, the oligomer is a fusion protein ...
The invention relates to compounds having agonist activity at the GLP-1 (glucagon-like-peptide 1) and GLP-2 (glucagon-like peptide 2) receptors. The compounds find use, inter alia, in the prophylaxis or treatment of intestinal damage and dysfunction, regulation of body weight, and prophylaxis ...