FFAR1 - Free fatty acid receptor 1 - human protein (Function)
 
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FFAR1 »  Free fatty acid receptor 1
 
Protein also known as:  G-protein coupled receptor 40.
Gene name:  FFAR1
Entry whose protein(s) existence is based on evidence at protein level
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1 36 1
GENE REF ISO

Function

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Overview 
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.  
5
  • UniProtKB
GO molecular function 
Bioactive lipid receptor activitydefinition[GO:0045125]  
1
  • UniProtKB
G-protein coupled receptor activitydefinition[GO:0004930]  
1
  • PINC
Lipid bindingdefinition[GO:0008289]  
1
  • UniProtKB KW
GO biological process 
G-protein coupled receptor signaling pathwaydefinition[GO:0007186]  
1
  • UniProtKB KW
Glucose homeostasisdefinition[GO:0042593] silver  
1
  • Ortholog Compara
Insulin secretiondefinition[GO:0030073] silver  
1
  • Ortholog Compara
Positive regulation of calcium ion transportdefinition[GO:0051928]  
1
  • UniProtKB
Response to fatty aciddefinition[GO:0070542]  
1
  • UniProtKB
Enzymatic activity 
It is regulated in the following manner
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 (PubMed21570468). 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 (PubMed24130766).  
3
  • UniProtKB
Pathways 
According to Reactome, this protein belongs to the following pathways:
Fatty Acids bound to GPR40 (FFAR1) regulate insulin secretion  REACT_19193  
Free fatty acid receptors  REACT_21268  
G alpha (q) signalling events  REACT_18283  
Synthesis, secretion, and inactivation of Glucagon-like Peptide-1 (GLP-1)  REACT_24019  
Synthesis, secretion, and inactivation of Glucose-dependent Insulinotropic Polypeptide (GIP)  REACT_23824  
 

Keywords

Molecular function 
G-protein coupled receptor  definition   [KW-0297]
Receptor  definition   [KW-0675]
Transducer  definition   [KW-0807]
Technical term 
Reference proteome  definition   [KW-1185]
 

Further external links

Other
GeneWiki: Free_fatty_acid_receptor_1
GenomeRNAi: 2864
PRO: PR:O14842
Chemistry
GuidetoPHARMACOLOGY: 225