Target Information

Target General Infomation
Target ID
T51385
Former ID
TTDI02509
Target Name
G-protein coupled receptor 120
Gene Name
FFAR4
Synonyms
Free fatty acid receptor 4; Gprotein coupled receptor 129; Gprotein coupled receptor GT01; Gprotein coupled receptor PGR4; Omega3 fatty acid receptor 1; FFAR4
Target Type
Research
Function
Receptor for medium and long-chain free fatty acids (FFAs). Signals via a G(q)/G(11)-coupled pathway. Acts as a receptor for omega-3 fatty acids and mediates robust anti- inflammatory effects, particularly in macrophages and fat cells. The anti-inflammatory effects involve inhibition of TAK1 through a beta-arrestin 2 (ARRB2)/TAB1-dependent effect, but independent of the G(q)/G(11)-coupled pathway. Mediates potent insulin sensitizing and antidiabetic effects by repressing macrophage- induced tissue inflammation. May mediate the taste of fatty acids. Mediates FFA-induced inhibition of apoptosis in enteroendocrine cells. May play a role in the regulation of adipocyte development and differentiation.
BioChemical Class
GPCR rhodopsin
UniProt ID
Q5NUL3
Sequence
MSPECARAAGDAPLRSLEQANRTRFPFFSDVKGDHRLVLAAVETTVLVLIFAVSLLGNVC
ALVLVARRRRRGATACLVLNLFCADLLFISAIPLVLAVRWTEAWLLGPVACHLLFYVMTL
SGSVTILTLAAVSLERMVCIVHLQRGVRGPGRRARAVLLALIWGYSAVAALPLCVFFRVV
PQRLPGADQEISICTLIWPTIPGEISWDVSFVTLNFLVPGLVIVISYSKILQTSEHLLDA
RAVVTHSEITKASRKRLTVSLAYSESHQIRVSQQDFRLFRTLFLLMVSFFIMWSPIIITI
LLILIQNFKQDLVIWPSLFFWVVAFTFANSALNPILYNMTLCRNEWKKIFCCFWFPEKGA
ILTDTSVKRNDLSIISG
Agonist alpha-linolenic acid Drug Info [529354]
compound A Drug Info [532872]
grifolic acid Drug Info [530168]
GW9508 Drug Info [529729]
NCG21 Drug Info [529803]
TUG-891 Drug Info [531880]
Pathways
WikiPathways Incretin Synthesis, Secretion, and Inactivation
GPCR ligand binding
References
Ref 529354Cloning and characterization of the rat free fatty acid receptor GPR120: in vivo effect of the natural ligand on GLP-1 secretion and proliferation of pancreatic beta cells. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jun;377(4-6):515-22.
Ref 529729Free fatty acid receptors and drug discovery. Biol Pharm Bull. 2008 Oct;31(10):1847-51.
Ref 529803Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists. J Med Chem. 2008 Dec 11;51(23):7640-4.
Ref 530168Novel selective ligands for free fatty acid receptors GPR120 and GPR40. Naunyn Schmiedebergs Arch Pharmacol. 2009 Sep;380(3):247-55.
Ref 531880Discovery of a potent and selective GPR120 agonist. J Med Chem. 2012 May 10;55(9):4511-5.
Ref 532872A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice. Nat Med. 2014 Aug;20(8):942-7.

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