Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET00GUR)
Name
Free fatty acid receptor 4 (FFAR4)
Synonyms    Click to Show/Hide the Synonyms of This DBT
G-protein coupled receptor 120; G-protein coupled receptor 129; G-protein coupled receptor GT01; G-protein coupled receptor PGR4; GPR129; Gprotein coupled receptor 129; Gprotein coupled receptor GT01; Gprotein coupled receptor PGR4; O3FAR1; Omega-3 fatty acid receptor 1; Omega3 fatty acid receptor 1; PGR4
Family G-protein coupled receptor (GPCR)  >>  G-protein coupled rhodopsin receptor (GPCR-A)
Organism
Homo sapiens (Human)
Gene Name FFAR4 Gene ID
338557
UniProt ID FFAR4_HUMAN (click to find more protein-related data of this DBT)
TTD ID T51385 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MSPECARAAGDAPLRSLEQANRTRFPFFSDVKGDHRLVLAAVETTVLVLIFAVSLLGNVC
ALVLVARRRRRGATACLVLNLFCADLLFISAIPLVLAVRWTEAWLLGPVACHLLFYVMTL
SGSVTILTLAAVSLERMVCIVHLQRGVRGPGRRARAVLLALIWGYSAVAALPLCVFFRVV
PQRLPGADQEISICTLIWPTIPGEISWDVSFVTLNFLVPGLVIVISYSKILQITKASRKR
LTVSLAYSESHQIRVSQQDFRLFRTLFLLMVSFFIMWSPIIITILLILIQNFKQDLVIWP
SLFFWVVAFTFANSALNPILYNMTLCRNEWKKIFCCFWFPEKGAILTDTSVKRNDLSIIS
G
Function
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.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Sodium stearate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Gelling agent; Glidant; Modified-release agent; Stiffening agent; lubricant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 1698.24 nM (estimated based on the structural similarity with CHEMBL4281719 ) [1]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Homo sapiens (Human)
                   UniProt ID FFAR4_HUMAN
          DIG Name: Lauric acid Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antifoaming agent; Emulsifying agent; Lubricant; Penetration agent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 7585.78 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID FFAR4_HUMAN
          DIG Name: Linoleic acid Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Penetration agent; Solubilizing agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 316.23 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID FFAR4_HUMAN
          DIG Name: Ricinoleic acid Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emollient; Emulsifying agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 1318.26 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID FFAR4_HUMAN
References
1 Succinct synthesis of saturated hydroxy fatty acids and in vitro evaluation of all hydroxylauric acids on FFA1, FFA4 and GPR84. Med Chem Comm. 2017; 8:1360-1365.
2 Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014 Jul 15; 24(14):3100-3.

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