GLP1R Membrane Protein Introduction

Introduction of GLP1R

The glucagon-like peptide 1 receptor (GLP1R) is a receptor protein encoded by gene GLP1R. GLP1R consists of two domains, an extracellular (ECD) that binds the C-terminal helix of GLP-1, and a transmembrane (TMD) domain that binds the N-terminal region of GLP-1. It was found on beta cells of the pancreas and involved in the control of blood sugar level by enhancing insulin secretion. It also stimulates glucose-induced insulin secretion.

Basic Information of GLP1R
Protein Name	Glucagon-like peptide 1 receptor
Gene Name	GLP1R
Aliases	GLP-1-R
Organism	Homo sapiens (Human)
UniProt ID>	P43220
Transmembrane Times	7
Length (aa)	463
Sequence	MAGAPGPLRLALLLLGMVGRAGPRPQGATVSLWETVQKWREYRRQCQRSLTEDPPPATDL FCNRTFDEYACWPDGEPGSFVNVSCPWYLPWASSVPQGHVYRFCTAEGLWLQKDNSSLPW RDLSECEESKRGERSSPEEQLLFLYIIYTVGYALSFSALVIASAILLGFRHLHCTRNYIH LNLFASFILRALSVFIKDAALKWMYSTAAQQHQWDGLLSYQDSLSCRLVFLLMQYCVAAN YYWLLVEGVYLYTLLAFSVLSEQWIFRLYVSIGWGVPLLFVVPWGIVKYLYEDEGCWTRN SNMNYWLIIRLPILFAIGVNFLIFVRVICIVVSKLKANLMCKTDIKCRLAKSTLTLIPLL GTHEVIFAFVMDEHARGTLRFIKLFTELSFTSFQGLMVAILYCFVNNEVQLEFRKSWERW RLEHLHIQRDSSMKPLKCPTSSLSSGATAGSSMYTATCQASCS

Function of GLP1R Membrane Protein

GLP1R is a receptor protein found on beta cells of the pancreas. This receptor, which functions at the cell surface, becomes internalized in response to GLP-1 and GLP-1 analogs, and it plays an important role in the signaling cascades leading to insulin secretion. Activated GLP1R stimulates the adenylyl cyclase pathway which results in increased insulin synthesis and release of insulin. GLP1R, expressed in the brain, is involved in the control of appetite. GLP1R, expressed in stretch responsive vagal neurons in the stomach and intestinesneurons, innervates stomach muscle and can communicate with additional organ systems changing breathing and heart rate due to activation.

Fig.1 Structure of protein GLP1R.

Application of GLP1R Membrane Protein in Literature

Sisley S., et al. Neuronal GLP1R mediates liraglutide’s anorectic but not glucose-lowering effect. The Journal of Clinical Investigation. 2014, 124(6): 2456–2463. PubMed ID: 24762441

This paper reports that glucose and body weight is regulated by the brain and the GLP1R mediator changes in neurons, but it is necessary for non-glucose reduction.
Ghosal S., et al. Disruption of Glucagon-Like Peptide 1 Signaling in Sim1 Neurons Reduces Physiological and Behavioral Reactivity to Acute and Chronic Stress. The Journal of Neuroscience. 2017, 37(1): 184–193. PubMed ID: 28053040

This paper proposes that glucagon-like peptide 1 (GLP-1) can mediate the global stress response in the hypothalamic paraventricular circulation.
Jia Y., et al. Exendin-4 ameliorates high glucose-induced fibrosis by inhibiting the secretion of miR-192 from injured renal tubular epithelial cells. Exp Mol Med. 2018. PubMed ID: 29717107

This article reveals that improvement in renal fibrosis is mediated by exendin-4 via the miR-192-GLP1R pathway.
Burmeister M.A., et al. Regulation of glucose kinetics during exercise by the glucagon-like peptide-1 receptor. The Journal of Physiology. 2012, 590(Pt 20): 5245–5255. PubMed ID: 22890715

This article shows that functional disruption of the Glp1r results in exercise-induced hyperglycemia associated with an excessive increase in glucagon secretion and HGP. These results suggest an essential role for basal Glp1r signaling in the suppression of alpha cell secretion during exercise.
Moon M.J., et al. Evolutionarily Conserved Residues at Glucagon-like Peptide-1 (GLP-1) Receptor Core Confer Ligand-induced Receptor Activation. Journal of Biological Chemistry. 2012, 287(6): 3873–3884. PubMed ID: 22105074

This article evaluates that glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) play important roles in insulin secretion through their receptors, GLP1R and GIPR.

GLP1R Preparation Options

To obtain the soluble and functional target protein, the versatile Magic™ membrane protein production platform in Creative Biolabs enables many flexible options, from which you can always find a better match for your particular project. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-GLP1R antibody development services.

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