This gene encodes a member of the GP40 family of G protein-coupled receptors that are clustered together on chromosome 19. The encoded protein is a receptor for medium and long chain free fatty acids and may be involved in the metabolic regulation of insulin secretion. Polymorphisms in this gene may be associated with type 2 diabetes. [provided by RefSeq, Apr 2009] See more...

Aliases for FFAR1 Gene

Aliases for FFAR1 Gene

  • Free Fatty Acid Receptor 1 2 3 4 5
  • G-Protein Coupled Receptor 40 3 4
  • FFA1R 2 3
  • GPR40 3 4
  • G Protein-Coupled Receptor 40 2
  • GPCR40 3
  • FFAR1 5

External Ids for FFAR1 Gene

Previous HGNC Symbols for FFAR1 Gene

  • GPR40

Previous GeneCards Identifiers for FFAR1 Gene

  • GC19P040535
  • GC19P035842
  • GC19P032350
  • GC19P035503
  • GC19P035513
  • GC19P037087
  • GC19P037260
  • GC19P037332
  • GC19P037804
  • GC19P035522
  • GC19P035541
  • GC19P036131
  • GC19P036264
  • GC19P036442
  • GC19P036614
  • GC19P036776
  • GC19P036925

Summaries for FFAR1 Gene

Entrez Gene Summary for FFAR1 Gene

  • This gene encodes a member of the GP40 family of G protein-coupled receptors that are clustered together on chromosome 19. The encoded protein is a receptor for medium and long chain free fatty acids and may be involved in the metabolic regulation of insulin secretion. Polymorphisms in this gene may be associated with type 2 diabetes. [provided by RefSeq, Apr 2009]

GeneCards Summary for FFAR1 Gene

FFAR1 (Free Fatty Acid Receptor 1) is a Protein Coding gene. Diseases associated with FFAR1 include Diabetes Mellitus, Noninsulin-Dependent. Among its related pathways are RET signaling and Integration of energy metabolism. Gene Ontology (GO) annotations related to this gene include G protein-coupled receptor activity and guanyl-nucleotide exchange factor activity. An important paralog of this gene is FFAR3.

UniProtKB/Swiss-Prot Summary for FFAR1 Gene

  • G-protein coupled receptor for medium and long chain saturated and unsaturated fatty acids that plays an important role in glucose homeostasis. Fatty acid binding increases glucose-stimulated insulin secretion, and may also enhance the secretion of glucagon-like peptide 1 (GLP-1). May also play a role in bone homeostasis; receptor signaling activates pathways that inhibit osteoclast differentiation (By similarity). Ligand binding leads to a conformation change that triggers signaling via G-proteins that activate phospholipase C, leading to an increase of the intracellular calcium concentration. Seems to act through a G(q) and G(i)-mediated pathway. Mediates the anti-inflammatory effects of omega-3 polyunsaturated fatty acids (PUFAs) via inhibition of NLRP3 inflammasome activation.

Tocris Summary for FFAR1 Gene

  • Free Fatty Acid (FFA) receptors are a group of Gq/11 protein-coupled receptors currently classified into FFA1, FFA2, FFA3 and FFA4 subtypes. FFA receptors are concentrated in pancreatic islet cells, immune cells and in the brain and are important in immunity and metabolism.

Gene Wiki entry for FFAR1 Gene

Additional gene information for FFAR1 Gene

No data available for CIViC Summary , PharmGKB "VIP" Summary , Rfam classification and piRNA Summary for FFAR1 Gene

Genomics for FFAR1 Gene

GeneHancer (GH) Regulatory Elements Pubs

Promoters and enhancers for FFAR1 Gene
- Elite GeneHancer and/or Elite GeneHancer-gene association Download GeneHancer data from 2017 publication | Request up-to-date GeneHancer data (full dataset)

GeneHancers around FFAR1 on the GeneHancer Hub at the UCSC Golden Path

Cistromic (ChIP-Seq) regulation report from SPP (The Signaling Pathways Project) for FFAR1

Top Transcription factor binding sites by QIAGEN in the FFAR1 gene promoter:
  • AML1a
  • Brachyury
  • GATA-2
  • GR
  • GR-alpha
  • GR-beta
  • NF-kappaB
  • NF-kappaB1

Genomic Locations for FFAR1 Gene

Genomic Locations for FFAR1 Gene
chr19:35,351,542-35,353,862
(GRCh38/hg38)
Size:
2,321 bases
Orientation:
Plus strand
chr19:35,842,445-35,843,367
(GRCh37/hg19)
Size:
923 bases
Orientation:
Plus strand

Genomic View for FFAR1 Gene

Genes around FFAR1 on UCSC Golden Path with GeneCards custom track

Cytogenetic band:
FFAR1 Gene in genomic location: bands according to Ensembl, locations according to GeneLoc (and/or Entrez Gene and/or Ensembl if different)
Genomic Location for FFAR1 Gene
GeneLoc Logo Genomic Neighborhood Exon StructureGene Density

RefSeq DNA sequence for FFAR1 Gene

Proteins for FFAR1 Gene

  • Protein details for FFAR1 Gene (UniProtKB/Swiss-Prot)

    Protein Symbol:
    O14842-FFAR1_HUMAN
    Recommended name:
    Free fatty acid receptor 1
    Protein Accession:
    O14842
    Secondary Accessions:
    • Q0VAS2
    • Q4VBL4

    Protein attributes for FFAR1 Gene

    Size:
    300 amino acids
    Molecular mass:
    31457 Da
    Quaternary structure:
    No Data Available

    Three dimensional structures from OCA and Proteopedia for FFAR1 Gene

neXtProt entry for FFAR1 Gene

Post-translational modifications for FFAR1 Gene

  • Glycosylation at Asn155
  • Modification sites at PhosphoSitePlus

Other Protein References for FFAR1 Gene

ENSEMBL proteins:
REFSEQ proteins:

No data available for DME Specific Peptides for FFAR1 Gene

Domains & Families for FFAR1 Gene

Gene Families for FFAR1 Gene

HGNC:
IUPHAR :
Human Protein Atlas (HPA):
  • FDA approved drug targets
  • G-protein coupled receptors
  • Predicted membrane proteins

Protein Domains for FFAR1 Gene

Suggested Antigen Peptide Sequences for FFAR1 Gene

GenScript: Design optimal peptide antigens:
  • G protein-coupled receptor 40 (A5Z1T7_HUMAN)
  • G-protein coupled receptor 40 (FFAR1_HUMAN)
  • FFAR1 protein (Q0IJ71_HUMAN)

Graphical View of Domain Structure for InterPro Entry

O14842

UniProtKB/Swiss-Prot:

FFAR1_HUMAN :
  • Belongs to the G-protein coupled receptor 1 family.
Family:
  • Belongs to the G-protein coupled receptor 1 family.
genes like me logo Genes that share domains with FFAR1: view

Function for FFAR1 Gene

Molecular function for FFAR1 Gene

UniProtKB/Swiss-Prot Function:
G-protein coupled receptor for medium and long chain saturated and unsaturated fatty acids that plays an important role in glucose homeostasis. Fatty acid binding increases glucose-stimulated insulin secretion, and may also enhance the secretion of glucagon-like peptide 1 (GLP-1). May also play a role in bone homeostasis; receptor signaling activates pathways that inhibit osteoclast differentiation (By similarity). Ligand binding leads to a conformation change that triggers signaling via G-proteins that activate phospholipase C, leading to an increase of the intracellular calcium concentration. Seems to act through a G(q) and G(i)-mediated pathway. Mediates the anti-inflammatory effects of omega-3 polyunsaturated fatty acids (PUFAs) via inhibition of NLRP3 inflammasome activation.
UniProtKB/Swiss-Prot EnzymeRegulation:
The receptor is strongly activated by gamma-linolenic acid, while myristate gives a lower response. It is also activated by phytanic acid and pristanic acid (PubMed:21570468). Is also activated by synthetic agonists, such as TAK-875 (fasiglifam); this compound is a partial agonist and potentiates the activity of the endogenous ligand gamma-linolenic acid (PubMed:24130766).

Phenotypes From GWAS Catalog for FFAR1 Gene

Gene Ontology (GO) - Molecular Function for FFAR1 Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0004930 G protein-coupled receptor activity TAS 9344866
GO:0008289 lipid binding IEA --
GO:0045125 bioactive lipid receptor activity IDA 24130766
genes like me logo Genes that share ontologies with FFAR1: view
genes like me logo Genes that share phenotypes with FFAR1: view

Animal Models for FFAR1 Gene

MGI Knock Outs for FFAR1:

Animal Model Products

CRISPR Products

Inhibitory RNA Products

  • Search GeneCopoeia for shRNA, lentivirus and/or AAV clone products for FFAR1

No data available for Enzyme Numbers (IUBMB) , Human Phenotype Ontology , Transcription Factor Targets and HOMER Transcription for FFAR1 Gene

Localization for FFAR1 Gene

Subcellular locations from UniProtKB/Swiss-Prot for FFAR1 Gene

Cell membrane. Multi-pass membrane protein.

Subcellular locations from

COMPARTMENTS
Extracellular space Cytosol Plasma membrane Cytoskeleton Lysosome Endosome Peroxisome ER Golgi Apparatus Nucleus Mitochondrion 0 1 2 3 4 5 Confidence
COMPARTMENTS Subcellular localization image for FFAR1 gene
Compartment Confidence
plasma membrane 5
extracellular 2
mitochondrion 2
peroxisome 2
nucleus 2
endoplasmic reticulum 2
cytosol 2
cytoskeleton 1
endosome 1
lysosome 1
golgi apparatus 1

Gene Ontology (GO) - Cellular Components for FFAR1 Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0005623 cell IEA --
GO:0005886 plasma membrane TAS --
GO:0005887 integral component of plasma membrane TAS,IDA 25043059
GO:0016020 membrane IEA --
GO:0016021 integral component of membrane IEA --
genes like me logo Genes that share ontologies with FFAR1: view

No data available for Subcellular locations from the Human Protein Atlas (HPA) for FFAR1 Gene

Pathways & Interactions for FFAR1 Gene

genes like me logo Genes that share pathways with FFAR1: view

SIGNOR curated interactions for FFAR1 Gene

Activates:

Gene Ontology (GO) - Biological Process for FFAR1 Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0007165 signal transduction IEA --
GO:0007186 G protein-coupled receptor signaling pathway TAS --
GO:0007204 positive regulation of cytosolic calcium ion concentration IDA 24742677
GO:0030073 insulin secretion IEA --
GO:0032024 positive regulation of insulin secretion IEA --
genes like me logo Genes that share ontologies with FFAR1: view

Drugs & Compounds for FFAR1 Gene

(25) Drugs for FFAR1 Gene - From: DrugBank, ApexBio, DGIdb, IUPHAR, HMDB, Tocris, and Novoseek

Name Status Disease Links Group Role Mechanism of Action Clinical Trials
linoleic acid Approved, Experimental Pharma Agonist, Full agonist, Activator, Pore Blocker, Channel blocker 0
Icosapent Approved Nutra Target, agonist Endogenous polyunsaturated fatty acid; stimulates ERK1/2 phosphorylation 0
Docosahexaenoic acid Approved, Investigational Pharma Agonist, Full agonist 0
oleic acid Approved, Investigational, Vet_approved Pharma Agonist, Full agonist, Activator, Activation 0
Palmitic Acid Approved Pharma Agonist, Full agonist 27

(3) Additional Compounds for FFAR1 Gene - From: IUPHAR and Novoseek

Name Synonyms Role CAS Number PubChem IDs PubMed IDs
TUG424
Agonist, Full agonist

(5) Tocris Compounds for FFAR1 Gene

Compound Action Cas Number
4-CMTB FFA2 agonist; also exhibits positive allosteric modulatory activity 300851-67-6
Grifolic acid Selective partial FFA4 (GPR120) agonist 80557-12-6
GW 9508 Potent and selective FFA1 (GPR40) agonist 885101-89-3
MEDICA 16 FFA1 (GPR40) agonist; also inhibits ATP citrate lyase 87272-20-6
TUG 891 Potent and selective FFA4 (GPR120) agonist 1374516-07-0

(9) ApexBio Compounds for FFAR1 Gene

Compound Action Cas Number
4-CMTB 300851-67-6
AS 2034178 Selective FFA1/GPR40 agonist 1030846-42-4
GSK1292263 Novel GPR119 agonist 1032823-75-8
GW-1100 GPR40 antagonist 306974-70-9
GW9508 FFA1/GPR40 agonist,potent and selective 885101-89-3
MEDICA 16 87272-20-6
TAK-875 GPR40 agonist 1000413-72-8
TUG 424 1082058-99-8
TUG-770 FFA1/GPR40 agonist 1402601-82-4
genes like me logo Genes that share compounds with FFAR1: view

Drug Products

Transcripts for FFAR1 Gene

mRNA/cDNA for FFAR1 Gene

1 REFSEQ mRNAs :
5 NCBI additional mRNA sequence :
1 Ensembl transcripts including schematic representations, and UCSC links to gene/alias where relevant :

CRISPR Products

Inhibitory RNA Products

  • Search GeneCopoeia for shRNA, lentivirus and/or AAV clone products for FFAR1

Alternative Splicing Database (ASD) splice patterns (SP) for FFAR1 Gene

No ASD Table

Relevant External Links for FFAR1 Gene

GeneLoc Exon Structure for
FFAR1

Expression for FFAR1 Gene

mRNA expression in normal human tissues from GTEx, Illumina, BioGPS, and SAGE for FFAR1 Gene

mRNA differential expression in normal tissues according to GTEx for FFAR1 Gene

This gene is overexpressed in Pancreas (x7.4), Ovary (x7.0), and Brain - Spinal cord (cervical c-1) (x6.2).

Transcriptomic regulation report from SPP (The Signaling Pathways Project) for FFAR1

SOURCE GeneReport for Unigene cluster for FFAR1 Gene:

Hs.248127

mRNA Expression by UniProt/SwissProt for FFAR1 Gene:

O14842-FFAR1_HUMAN
Tissue specificity: Detected in brain and pancreas. Detected in pancreatic beta cells.

Evidence on tissue expression from TISSUES for FFAR1 Gene

  • Pancreas(2.9)
  • Intestine(2.3)
  • Blood(2.2)
  • Nervous system(2.1)
  • Liver(2.1)
genes like me logo Genes that share expression patterns with FFAR1: view

No data available for mRNA expression in embryonic tissues and stem cells from LifeMap Discovery , Protein differential expression in normal tissues , Protein expression , Protein tissue co-expression partners and Phenotype-based relationships between genes and organs from Gene ORGANizer for FFAR1 Gene

Orthologs for FFAR1 Gene

This gene was present in the common ancestor of chordates.

Orthologs for FFAR1 Gene

Organism Taxonomy Gene Similarity Type Details
Chimpanzee
(Pan troglodytes)
Mammalia FFAR1 30 31
  • 99.56 (n)
OneToOne
Dog
(Canis familiaris)
Mammalia FFAR1 30 31
  • 85.4 (n)
OneToOne
Cow
(Bos Taurus)
Mammalia FFAR1 31
  • 84 (a)
OneToOne
Mouse
(Mus musculus)
Mammalia Ffar1 30 17 31
  • 79.33 (n)
OneToOne
Rat
(Rattus norvegicus)
Mammalia Ffar1 30
  • 78.33 (n)
Oppossum
(Monodelphis domestica)
Mammalia FFAR1 31
  • 71 (a)
OneToOne
Lizard
(Anolis carolinensis)
Reptilia FFAR1 31
  • 34 (a)
OneToOne
Zebrafish
(Danio rerio)
Actinopterygii FFAR1 31
  • 34 (a)
OneToOne
Species where no ortholog for FFAR1 was found in the sources mined by GeneCards:
  • A. gosspyii yeast (Eremothecium gossypii)
  • Actinobacteria (Mycobacterium tuberculosis)
  • African clawed frog (Xenopus laevis)
  • African malaria mosquito (Anopheles gambiae)
  • Alicante grape (Vitis vinifera)
  • Alpha proteobacteria (Wolbachia pipientis)
  • Amoeba (Dictyostelium discoideum)
  • Archea (Pyrococcus horikoshii)
  • Baker's yeast (Saccharomyces cerevisiae)
  • Barley (Hordeum vulgare)
  • Beta proteobacteria (Neisseria meningitidis)
  • Bread mold (Neurospora crassa)
  • Chicken (Gallus gallus)
  • Chromalveolata (Phytophthora infestans)
  • Common water flea (Daphnia pulex)
  • Corn (Zea mays)
  • E. coli (Escherichia coli)
  • Filamentous fungi (Aspergillus nidulans)
  • Firmicute Bacteria (Streptococcus pneumoniae)
  • Fission Yeast (Schizosaccharomyces pombe)
  • Fruit Fly (Drosophila melanogaster)
  • Green Algae (Chlamydomonas reinhardtii)
  • Honey Bee (Apis mellifera)
  • K. Lactis Yeast (Kluyveromyces lactis)
  • Loblloly Pine (Pinus taeda)
  • Malaria Parasite (Plasmodium falciparum)
  • Medicago Trunc (Medicago Truncatula)
  • Moss (Physcomitrella patens)
  • Orangutan (Pongo pygmaeus)
  • Pig (Sus scrofa)
  • Platypus (Ornithorhynchus anatinus)
  • Rainbow Trout (Oncorhynchus mykiss)
  • Rice (Oryza sativa)
  • Rice Blast Fungus (Magnaporthe grisea)
  • Schistosome Parasite (Schistosoma mansoni)
  • Sea Anemone (Nematostella vectensis)
  • Sea Vase (Ciona intestinalis)
  • Sea Squirt (Ciona savignyi)
  • Sea Urchin (Strongylocentrotus purpuratus)
  • Sorghum (Sorghum bicolor)
  • Soybean (Glycine max)
  • Stem Rust Fungus (Puccinia graminis)
  • Sugarcane (Saccharum officinarum)
  • Thale Cress (Arabidopsis thaliana)
  • Tomato (Lycopersicon esculentum)
  • Toxoplasmosis (Toxoplasma gondii)
  • Trichoplax (Trichoplax adhaerens)
  • Tropical Clawed Frog (Silurana tropicalis)
  • Wheat (Triticum aestivum)
  • Worm (Caenorhabditis elegans)

Evolution for FFAR1 Gene

ENSEMBL:
Gene Tree for FFAR1 (if available)
TreeFam:
Gene Tree for FFAR1 (if available)
Aminode:
Evolutionary constrained regions (ECRs) for FFAR1: view image

Paralogs for FFAR1 Gene

(4) SIMAP similar genes for FFAR1 Gene using alignment to 2 proteins:

  • FFAR1_HUMAN
  • Q0IJ71_HUMAN
genes like me logo Genes that share paralogs with FFAR1: view

Variants for FFAR1 Gene

Sequence variations, with clinical significance, from ClinVar and Humsavar, with links to dbSNP for FFAR1 Gene

SNP ID Clinical significance and condition Chr 19 pos Variation AA Info Type
rs2301151 - p.Arg211His

Additional dbSNP identifiers (rs#s) for FFAR1 Gene

Structural Variations from Database of Genomic Variants (DGV) for FFAR1 Gene

Variant ID Type Subtype PubMed ID
esv2718493 CNV deletion 23290073
esv2758758 CNV loss 17122850
nsv1067129 CNV loss 25217958
nsv1160606 CNV deletion 26073780
nsv173 CNV deletion 15895083
nsv2471 CNV deletion 18451855
nsv510765 CNV deletion 20534489
nsv833810 CNV gain 17160897

Variation tolerance for FFAR1 Gene

Gene Damage Index Score: 1.59; 30.70% of all genes are more intolerant (likely to be disease-causing)

Additional Variant Information for FFAR1 Gene

Human Gene Mutation Database (HGMD)
FFAR1
SNPedia medical, phenotypic, and genealogical associations of SNPs for
FFAR1

SNP Genotyping and Copy Number Assay Products

No data available for Polymorphic Variants from UniProtKB/Swiss-Prot for FFAR1 Gene

Disorders for FFAR1 Gene

MalaCards: The human disease database

(1) MalaCards diseases for FFAR1 Gene - From: DISEASES

Disorder Aliases PubMed IDs
diabetes mellitus, noninsulin-dependent
  • niddm
- elite association - COSMIC cancer census association via MalaCards
Search FFAR1 in MalaCards View complete list of genes associated with diseases

Additional Disease Information for FFAR1

Genetic Association Database
(GAD)
Human Genome Epidemiology Navigator
(HuGE)
ATLAS of Genetics and Cytogenetics in Oncology and Haematology
Open Targets Platform
genes like me logo Genes that share disorders with FFAR1: view

No data available for UniProtKB/Swiss-Prot and Genatlas for FFAR1 Gene

Publications for FFAR1 Gene

  1. Two arginine-glutamate ionic locks near the extracellular surface of FFAR1 gate receptor activation. (PMID: 19068482) Sum CS … Gershengorn MC (The Journal of biological chemistry 2009) 3 4 23
  2. Loss-of-function mutation of the GPR40 gene associates with abnormal stimulated insulin secretion by acting on intracellular calcium mobilization. (PMID: 18583466) Vettor R … Frittitta L (The Journal of clinical endocrinology and metabolism 2008) 3 23 41
  3. Studies of relationships between variation of the human G protein-coupled receptor 40 Gene and Type 2 diabetes and insulin release. (PMID: 15606695) Hamid YH … Hansen T (Diabetic medicine : a journal of the British Diabetic Association 2005) 3 23 41
  4. GPR40 gene Arg211His polymorphism may contribute to the variation of insulin secretory capacity in Japanese men. (PMID: 15736105) Ogawa T … Saruta T (Metabolism: clinical and experimental 2005) 3 23 41
  5. Structural basis for GPR40 allosteric agonism and incretin stimulation. (PMID: 29695780) Ho JD … Hamdouchi C (Nature communications 2018) 3 4

Products for FFAR1 Gene

  • Addgene plasmids for FFAR1
  • Signalway ELISA kits for FFAR1
  • Signalway Proteins for FFAR1

Sources for FFAR1 Gene