Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0VW3D)
Name
Free fatty acid receptor 1 (FFAR1)
Synonyms    Click to Show/Hide the Synonyms of This DBT
G-protein coupled receptor 40; FFAR1; Gprotein coupled receptor 40
Family G-protein coupled receptor (GPCR)  >>  G-protein coupled rhodopsin receptor (GPCR-A)
Organism
Homo sapiens (Human)
Gene Name FFAR1 Gene ID
2864
UniProt ID FFAR1_HUMAN (click to find more protein-related data of this DBT)
TTD ID T25608 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MDLPPQLSFGLYVAAFALGFPLNVLAIRGATAHARLRLTPSLVYALNLGCSDLLLTVSLP
LKAVEALASGAWPLPASLCPVFAVAHFFPLYAGGGFLAALSAGRYLGAAFPLGYQAFRRP
CYSWGVCAAIWALVLCHLGLVFGLEAPGGWLDHSNTSLGINTPVNGSPVCLEAWDPASAG
PARFSLSLLLFFLPLAITAFCYVGCLRALARSGLTHRRKLRAAWVAGGALLTLLLCVGPY
NASNVASFLYPNLGGSWRKLGLITGAWSVVLNPLVTGYLGRGPGLKTVCAARTQGGKSQK
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. Ligand binding leads to a conformation change that triggers signaling via G-proteins that activate phospholipase C.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Hydroxystearic 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
Other agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 6760.83 nM (estimated based on the structural similarity with CHEMBL4278254 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.958333333
                   Tested Species Homo sapiens (Human)
                   UniProt ID FFAR1_HUMAN
          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 = 20892.96 nM (estimated based on the structural similarity with CHEMBL4281719 ) [1]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Homo sapiens (Human)
                   UniProt ID FFAR1_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 = 758.58 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID FFAR1_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 = 540 nM (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID FFAR1_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 = 11481.54 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID FFAR1_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 Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer. J Med Chem. 2016 May 26; 59(10):4849-58.
3 Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists. Bioorg Med Chem Lett. 2008 Dec 15; 18(24):6357-61.

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