GPR119 Membrane Protein Introduction

Introduction of GPR119

The GPR119 receptor is a member of the G-protein-coupled receptor superfamily. It is a type A rhodopsin isolated G protein-coupled receptor that has seven transmembrane regions in its structure. GPR119 is coupled to G protein in the cytoplasm by G protein 3 subunits (α, β, γ). The GPCR peptide consists of seven transmembrane alpha helices at the N-terminus, three extracellular loops at the C-terminus, and three to four intracellular loops at the C-terminus. The N-terminus is extracellular and is often glycosylated; the C-terminus is intracellular and most likely phosphorylates; seven transmembrane alpha helices repeatedly cross the lipid bilayer of the cell membrane. In humans, GPR119 is mainly distributed on the surface of pancreatic β cells, liver and gastrointestinal endocrine cells.

Basic Information of GPR119
Protein Name	Glucose-dependent insulinotropic receptor
Gene Name	GPR119
Aliases	GPCR2, G protein-coupled receptor 119
Organism	Homo sapiens (Human)
UniProt ID	Q8TDV5
Transmembrane Times	7
Length (aa)	335
Sequence	MESSFSFGVILAVLASLIIATNTLVAVAVLLLIHKNDGVSLCFTLNLAVADTLIGVAISGLLTDQLSSPSRPTQKTLCSLRMAFVTSSAAASVLTVMLITFDRYLAIKQPFRYLKIMSGFVAGACIAGLWLVSYLIGFLPLGIPMFQQTAYKGQCSFFAVFHPHFVLTLSCVGFFPAMLLFVFFYCDMLKIASMHSQQIRKMEHAGAMAGGYRSPRTPSDFKALRTVSVLIGSFALSWTPFLITGIVQVACQECHLYLVLERYLWLLGVGNSLLNPLIYAYWQKEVRLQLYHMALGVKKVLTSFLLFLSARNCGPERPRESSCHIVTISSSEFDG

Function of GPR119 Membrane Protein

GPR119 can combine with Oleylethanolamide (OEA), Monoglyceride (2OG) and Cannabinoids, promote GLP-1 and GIP levels in vivo, proliferate islet beta cells, promote insulin secretion, reduce appetite, delay gastric row empty, so that glucose-dependent stimulation of insulin release increased, lowering blood sugar while suppressing appetite and weight loss. Studies have shown that the G protein is adsorbed on the inner surface of the cell membrane. When the agonist binds with GPR119, the protein stimulates the protein to increase the intracellular cyclic adenosine monophosphate concentration and stimulate intracellular stimulation-secretion coupling, thereby increasing hormone secretion.

Fig.1 The structure of GPR119 membrane protein.

Application of GPR119 in Literature

Arifin S.A., et al. Oleoyl-lysophosphatidylinositol enhances glucagon-like peptide-1 secretion from enteroendocrine L-cells through GPR119. Biochim Biophys Acta. 2018. PubMed ID: 29883799

This article reports that GPR119 is a receptor for Oleoyl-LPI, upstream of ERK1/2 and cAMP/PKA/CREB pathways, and that Oleoyl-LPI can mediate GLP-1 secretion via GPR119.
Li N.X., et al. GPR119 Agonism Increases Glucagon Secretion During Insulin-Induced Hypoglycemia. Diabetes. 2018, 67(7): 1401-1413. PubMed ID: 29669745

This article reveals that GPR119 agonists have the ability to pharmacologically augment glucagon secretion, particularly in response to hypoglycemia in diabetic rodents.
Kato M., et al. Safety and Pharmacokinetics of DS-8500a, a Novel GPR119 Agonist, After Multiple Oral Doses in Healthy Japanese Males. Clin Drug Investig. 2018, 38(6): 519-525. PubMed ID: 29582248

The article evaluates the safety and pharmacokinetics of DS-8500a (GPR119 agonist) in healthy adult Japanese male subjects under fed conditions.
Harada K., et al. Design and synthesis of novel and potent GPR119 agonists with a spirocyclic structure. Bioorg Med Chem Lett. 2018, 28(7): 1228-1233. PubMed ID: 29519733

This article reports that they have found some novel spirocyclohexane derivatives by exploring alternative structures for the characteristically substituted piperidine or piperazine rings in GPR119 agonists.
Yamada Y., et al. Efficacy and Safety of GPR119 Agonist DS-8500a in Japanese Patients with Type 2 Diabetes: a Randomized, Double-Blind, Placebo-Controlled, 12-Week Study. Adv Ther. 2018, 35(3): 367-381. PubMed ID: 29488152

This article shows that DS-8500a has a significant effect on glucose reduction in Japanese T2DM patients with a therapeutic effect of up to 12 weeks and is well tolerated.

GPR119 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-GPR119 antibody development services.

As a forward-looking research institute as well as a leading customer service provider in the field of membrane protein, Creative Biolabs has won good reputation among our worldwide customers for successfully accomplishing numerous challenging projects including generation of many functional membrane proteins. Please feel free to contact us for more information.

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