Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET07ECZ)
Name
Free fatty acid receptor 2 (FFAR2)
Synonyms    Click to Show/Hide the Synonyms of This DBT
G-protein coupled receptor 43; Leukocyte-specific STAT-induced GPCR; FFAR2; Gprotein coupled receptor 43
Family G-protein coupled receptor (GPCR)  >>  G-protein coupled rhodopsin receptor (GPCR-A)
Organism
Homo sapiens (Human)
Gene Name FFAR2 Gene ID
2867
UniProt ID FFAR2_HUMAN (click to find more protein-related data of this DBT)
TTD ID T28213 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MLPDWKSSLILMAYIIIFLTGLPANLLALRAFVGRIRQPQPAPVHILLLSLTLADLLLLL
LLPFKIIEAASNFRWYLPKVVCALTSFGFYSSIYCSTWLLAGISIERYLGVAFPVQYKLS
RRPLYGVIAALVAWVMSFGHCTIVIIVQYLNTTEQVRSGNEITCYENFTDNQLDVVLPVR
LELCLVLFFIPMAVTIFCYWRFVWIMLSQPLVGAQRRRRAVGLAVVTLLNFLVCFGPYNV
SHLVGYHQRKSPWWRSIAVVFSSLNASLDPLLFYFSSSVVRRAFGRGLQVLRNQGSSLLG
RRGKDTAEGTNEDRGVGQGEGMPSSDFTTE
Function
G protein-coupled receptor that is activated by a major product of dietary fiber digestion, the short chain fatty acids (SCFAs), and that plays a role in the regulation of whole-body energy homeostasis and in intestinal immunity. In omnivorous mammals, the short chain fatty acids acetate, propionate and butyrate are produced primarily by the gut microbiome that metabolizes dietary fibers. SCFAs serve as a source of energy but also act as signaling molecules.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Acetic 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
Acidulant; Buffering agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 120000 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID FFAR2_HUMAN
          DIG Name: Ammonium acetate 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
Buffering agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 250000 nM (estimated based on the structural similarity with CHEMBL539 ) [2]
                   Structural Similarity Tanimoto coefficient = 0.8
                   Tested Species Homo sapiens (Human)
                   UniProt ID FFAR2_HUMAN
          DIG Name: Propionic 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
Acidulant; Antimicrobial preservative; Antioxidant
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 130000 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID FFAR2_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 251188.64 nM (tested by experiment) [3]
                   Tested Species Mus musculus (Mouse)
                   UniProt ID FFAR2_MOUSE
References
1 The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators. Bioorg Med Chem Lett. 2010 Jan 15; 20(2):493-8.
2 Microbiota-Host Transgenomic Metabolism, Bioactive Molecules from the Inside. J Med Chem. 2018 Jan 11; 61(1):47-61.
3 Discovery of a Potent Thiazolidine Free Fatty Acid Receptor 2 Agonist with Favorable Pharmacokinetic Properties. J Med Chem. 2018 Nov 8; 61(21):9534-9550.

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