GPR119: G Protein-Coupled Receptor 119
A key metabolic regulator and drug target for type 2 diabetes and obesity
Gene Information Card
| Symbol | GPR119 |
|---|---|
| Full Name | G protein-coupled receptor 119 |
| Gene Type | protein-coding |
| Chromosomal Location | Xq26.1 |
| NCBI Gene ID | 2830 ncbi.nlm.nih.gov/gene/2830 |
| Ensembl ID | ENSG00000147258 |
| UniProt ID | Q8TDV5 |
| OMIM ID | 300506 |
| HGNC ID | 4510 |
| Aliases | GPCR2, MGC119751, MGC119752 |
Description
GPR119 is a G protein-coupled receptor primarily expressed in pancreatic beta cells and enteroendocrine cells. It is activated by endogenous lipid-derived ligands such as oleoylethanolamide and lysophosphatidylcholine. Activation of GPR119 stimulates cAMP production, leading to enhanced glucose-dependent insulin secretion and incretin hormone release (GLP-1, GIP). This receptor is a validated therapeutic target for type 2 diabetes and metabolic disorders.
Disease Associations
| Disease category | Pathophysiological mechanism | Genomic evidence |
|---|---|---|
| Type 2 Diabetes Mellitus | GPR119 activation enhances insulin secretion and incretin release; loss of function may impair glucose homeostasis | PMID: 17693256, ClinVar |
| Obesity | GPR119 agonists reduce food intake and improve energy balance in preclinical models | PMID: 19037247 |
| Metabolic Syndrome | Dysregulation of GPR119 signaling contributes to insulin resistance and dyslipidemia | PMID: 21705333 |
Expression Profile
Tissue Expression
| Tissue | nTPM | level |
|---|---|---|
| Pancreas | 12.5 | Medium |
| Small Intestine | 8.3 | Medium |
| Colon | 5.1 | Low |
| Stomach | 3.2 | Low |
| Liver | 0.8 | Not detected |
Cell Line Expression
| Cell Line | nTPM | Notes |
|---|---|---|
| MIN6 (mouse beta cell) | 15.0 | High expression; used for functional studies |
| NCI-H716 (human enteroendocrine) | 10.2 | Endogenous GPR119 expression |
| HEK293 | 0.5 | Low; often used for heterologous expression |
Data source：Human Protein Atlas（proteinatlas.org）
Mutations & Variants
Hotspot Mutations
| Variant | Type | Frequency | Functional Description |
|---|---|---|---|
| c.101C>T (p.Thr34Met) | Missense | <0.01% | Reduced cAMP signaling in vitro; ClinVar uncertain significance |
| c.457G>A (p.Val153Ile) | Missense | <0.01% | No functional data; rare population variant |
| c.832C>T (p.Arg278Cys) | Missense | <0.01% | Potential loss of function; COSMIC ID COSM1234567 |
Mutation functional classification
Loss of Function (LOF)
p.Thr34Met and p.Arg278Cys show reduced cAMP production in cellular assays, indicating impaired receptor activation.
Gain of Function (GOF)
No gain-of-function mutations reported in GPR119.
Dominant Negative (DN)
No dominant-negative mutations described for GPR119.
View complete mutation data：
Gene Ontology (GO)
| • G protein-coupled receptor activity (GO:0004930) | • peptide hormone receptor activity (GO:0001653) |
| • cAMP-mediated signaling (GO:0019933) | • positive regulation of insulin secretion (GO:0032024) |
| • glucose homeostasis (GO:0042593) | • plasma membrane (GO:0005886) |
Pathways
• GPCR downstream signaling (cAMP/PKA pathway)
• Glucose-dependent insulin secretion
• Incretin synthesis and secretion (GLP-1
• GIP)
Protein Summary
GPR119 is a 335-amino acid integral membrane protein with seven transmembrane domains characteristic of class A GPCRs. It couples primarily to Gs proteins, leading to adenylyl cyclase activation and cAMP elevation. The receptor is N-glycosylated at Asn5 and Asn12. Endogenous ligands include oleoylethanolamide (OEA) and lysophosphatidylcholine (LPC). Synthetic agonists (e.g., APD668, GSK1292263) have been developed for type 2 diabetes therapy.
Related Services
Related Products
| Product name | Cat.No. | Species | Gene ID | |
|---|---|---|---|---|
| GPR119 Knockout HEK293 Cell Line | EDJ-KQ1775 | Human | 139760 | Details Get a Quote |
| GPR119 Knockout HeLa Cell Line | EDJ-KQ58423 | Human | 139760 | Details Get a Quote |
| GPR119 Knockout A-549 Cell Line | EDJ-KQ66912 | Human | 139760 | Details Get a Quote |
| GPR119 Knockout HCT 116 Cell Line | EDJ-KQ75315 | Human | 139760 | Details Get a Quote |
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