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10 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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FFAR2
free fatty acid receptor 2
Chromosome 19 · 19q13.12
NCBI Gene: 2867Ensembl: ENSG00000126262.5HGNC: HGNC:4501UniProt: C6KYL4
73PubMed Papers
20Diseases
1Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
CLINICAL
Clinical Trials
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
G protein-coupled receptor activitycell surface pattern recognition receptor signaling pathwaypositive regulation of interleukin-8 productionprotein bindingtype 1 diabetes mellitusulcerative colitisSepsisAlzheimer disease
✦AI Summary

FFAR2 (GPR43) is a G protein-coupled receptor activated by short-chain fatty acids (SCFAs)—acetate, propionate, and butyrate—produced by gut microbiota fermentation of dietary fiber 1. Upon SCFA binding, FFAR2 couples to Gi/o and Gq proteins, triggering calcium mobilization, MAPK phosphorylation, and cAMP inhibition 1. The receptor exhibits constitutive activity independent of SCFA binding. FFAR2 regulates energy homeostasis by modulating GLP-1 and leptin secretion, controlling glucose metabolism and adipogenesis 1. Critically, FFAR2 maintains intestinal immune tolerance by promoting regulatory T cell (Treg) differentiation and colonic Treg homeostasis in an SCFA-dependent manner, protecting against colitis 2. The receptor also mediates immune responses by regulating chemokine and cytokine production, with implications for inflammatory bowel disease pathogenesis and treatment 3. In cancer, FFAR2 expressed on myeloid-derived suppressor cells drives immunosuppression through acetic acid signaling via Gαq/calcium/PPAR-γ/Arg1 axes, promoting L-arginine depletion and T cell dysfunction 4. FFAR2 inhibition enhances anti-tumor CD8+ T cell responses and overcomes checkpoint blockade resistance 4. Additionally, FFAR2 mediates butyrate-induced ferroptosis in tumor cells via mTOR signaling 5, suggesting dual therapeutic potential in cancer immunotherapy and treatment.

Sources cited
1
FFAR2 is activated by SCFAs (acetate, butyrate, propionate), couples to Gi/o and Gq proteins, and regulates metabolism and immune responses
PMID: 31487233
2
FFAR2 is required for SCFA-mediated regulation of colonic Treg homeostasis and protection against colitis
PMID: 23828891
3
FFAR2 (GPR43) mediates SCFA signaling for intestinal homeostasis and has relevance to inflammatory bowel disease pathogenesis
PMID: 30915065
4
Butyrate activates FFAR2 to promote ferroptosis through FFAR2-mTORC1 signaling in tumor cells
PMID: 37185889
5
FFAR2 on myeloid-derived suppressor cells drives cancer immunosuppression via acetic acid/Gαq/calcium/PPAR-γ/Arg1 axis; FFAR2 inhibition enhances anti-tumor immunity
PMID: 38402237
Disease Associationsⓘ20
type 1 diabetes mellitusOpen Targets
0.09Suggestive
ulcerative colitisOpen Targets
0.09Suggestive
SepsisOpen Targets
0.09Suggestive
Alzheimer diseaseOpen Targets
0.08Suggestive
neoplasmOpen Targets
0.08Suggestive
atrial fibrillationOpen Targets
0.08Suggestive
hyperinsulinism due to INSR deficiencyOpen Targets
0.08Suggestive
MODYOpen Targets
0.08Suggestive
graft versus host diseaseOpen Targets
0.08Suggestive
abortionOpen Targets
0.07Suggestive
hyperproinsulinemiaOpen Targets
0.07Suggestive
acute myocardial infarctionOpen Targets
0.07Suggestive
hyperinsulinism due to glucokinase deficiencyOpen Targets
0.07Suggestive
liver dysplastic noduleOpen Targets
0.07Suggestive
gestational diabetesOpen Targets
0.07Suggestive
goutOpen Targets
0.07Suggestive
colorectal carcinomaOpen Targets
0.07Suggestive
exercise-induced hyperinsulinismOpen Targets
0.06Suggestive
isolated agammaglobulinemiaOpen Targets
0.06Suggestive
arterial embolismOpen Targets
0.06Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets1
GLPG-0974Phase II
Free fatty acid receptor 2 antagonist
abortion
Related Genes
NPYProtein interaction98%FFAR4Protein interaction96%GCGProtein interaction96%SSTProtein interaction95%PYYProtein interaction90%GPR84Protein interaction83%
Tissue Expression6 tissues
Bone Marrow
100%
Lung
98%
Liver
12%
Brain
7%
Heart
4%
Ovary
2%
Gene Interaction Network
Click a node to explore
FFAR2NPYFFAR4GCGSSTPYYGPR84
PROTEIN STRUCTURE
Preparing viewer…
PDB8J24 · 2.60 Å · EM
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
1.72LoF Tolerant
pLIⓘ
0.41Tolerant
Observed/Expected LoF0.00 [0.00–1.72]
RankingsWhere FFAR2 stands among ~20K protein-coding genes
  • #6,462of 20,598
    Most Researched73
  • #16,198of 17,882
    Most Constrained (LOEUF)1.72
Genes detectedFFAR2
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
Free Fatty Acid Receptors in Health and Disease.
PMID: 31487233
Physiol Rev · 2020
1.00
2
The microbial metabolites, short-chain fatty acids, regulate colonic Treg cell homeostasis.
PMID: 23828891
Science · 2013
0.90
3
Short Chain Fatty Acids (SCFAs)-Mediated Gut Epithelial and Immune Regulation and Its Relevance for Inflammatory Bowel Diseases.
PMID: 30915065
Front Immunol · 2019
0.80
4
Butyrate dictates ferroptosis sensitivity through FFAR2-mTOR signaling.
PMID: 37185889
Cell Death Dis · 2023
0.70
5
Trans-vaccenic acid reprograms CD8
PMID: 37993715
Nature · 2023
0.60