Names & Taxonomy

Uniprot ID:
O14842
Entry Name:
FFAR1_HUMAN
Status:
reviewed
Protein Names:
Free fatty acid receptor 1 (G-protein coupled receptor 40)
Gene Names:
FFAR1 GPR40
Gene Names Primary:
FFAR1
Organism:
Homo sapiens (Human)

Structure

Length:
300
Sequence:
MDLPPQLSFGLYVAAFALGFPLNVLAIRGATAHARLRLTPSLVYALNLGCSDLLLTVSLPLKAVEALASGAWPLPASLCPVFAVAHFFPLYAGGGFLAALSAGRYLGAAFPLGYQAFRRPCYSWGVCAAIWALVLCHLGLVFGLEAPGGWLDHSNTSLGINTPVNGSPVCLEAWDPASAGPARFSLSLLLFFLPLAITAFCYVGCLRALARSGLTHRRKLRAAWVAGGALLTLLLCVGPYNASNVASFLYPNLGGSWRKLGLITGAWSVVLNPLVTGYLGRGPGLKTVCAARTQGGKSQK
Proteomes:
UP000005640

Subcellular location

Subcellular Location:
Cell membrane

Function

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.
Enzyme Regulation:
ENZYME REGULATION: 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).
Cross Reference Drug Bank:
DB00159
Gene Ontology Go:
integral component of plasma membrane
plasma membrane
bioactive lipid receptor activity
G-protein coupled receptor activity
guanyl-nucleotide exchange factor activity
lipid binding
energy reserve metabolic process
G-protein coupled receptor signaling pathway
glucose homeostasis
insulin secretion
positive regulation of calcium ion transport
positive regulation of GTPase activity
positive regulation of insulin secretion
regulation of insulin secretion
response to fatty acid
small molecule metabolic process
Gene Ontology Biological Process:
energy reserve metabolic process
glucose homeostasis
G-protein coupled receptor signaling pathway
insulin secretion
positive regulation of calcium ion transport
positive regulation of GTPase activity
positive regulation of insulin secretion
regulation of insulin secretion
response to fatty acid
small molecule metabolic process
Gene Ontology Molecular Function:
bioactive lipid receptor activity
G-protein coupled receptor activity
guanyl-nucleotide exchange factor activity
lipid binding
Gene Ontology Cellular Component:
integral component of plasma membrane
plasma membrane
Keywords:
3D-structure
Cell membrane
Complete proteome
Disulfide bond
G-protein coupled receptor
Glycoprotein
Lipid-binding
Membrane
Polymorphism
Receptor
Reference proteome
Transducer
Transmembrane
Transmembrane helix

Publication

PubMed ID:
9344866 15489334 12496284 16289108 17699519 19068482 21570468 24130766 25043059