Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET08PHI)
Name
GPCR84 receptor (GPR84)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Inflammation-related GPCR EX33; EX33; G-protein coupled receptor 84; Inflammation-related G-protein coupled receptor EX33
Family G-protein coupled receptor (GPCR)  >>  G-protein coupled rhodopsin receptor (GPCR-A)
Organism
Homo sapiens (Human)
Gene Name GPR84 Gene ID
53831
UniProt ID GPR84_HUMAN (click to find more protein-related data of this DBT)
TTD ID T98091 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MWNSSDANFSCYHESVLGYRYVAVSWGVVVAVTGTVGNVLTLLALAIQPKLRTRFNLLIA
NLTLADLLYCTLLQPFSVDTYLHLHWRTGATFCRVFGLLLFASNSVSILTLCLIALGRYL
LIAHPKLFPQVFSAKGIVLALVSTWVVGVASFAPLWPIYILVPVVCTCSFDRIRGRPYTT
ILMGIYFVLGLSSVGIFYCLIHRQVKRAAQALDQYKLRQASIHSNHVARTDEAMPGRFQE
LDSRLASGGPSEGISSEPVSAATTQTLEGDSSEVGDQINSKRAKQMAEKSPPEASAKAQP
IKGARRAPDSSSEFGKVTRMCFAVFLCFALSYIPFLLLNILDARVQAPRVVHMLAANLTW
LNGCINPVLYAAMNRQFRQAYGSILKRGPRSFHRLH
Function
Receptor for medium-chain free fatty acid (FFA) with carbon chain lengths of C9 to C14. Capric acid (C10:0), undecanoic acid (C11:0) and lauric acid (C12:0) are the most potent agonists. Not activated by short-chain and long-chain saturated and unsaturated FFAs. Activation by medium-chain free fatty acid is coupled to a pertussis toxin sensitive G(i/o) protein pathway. May have important roles in processes from fatty acid metabolism to regulation of the immune system.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Caprylic 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; Flavoring agent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 19600 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID GPR84_HUMAN
          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 = 3860 nM (estimated based on the structural similarity with CHEMBL2004471 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.958333333
                   Tested Species Homo sapiens (Human)
                   UniProt ID GPR84_HUMAN
          DIG Name: Myristic 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; lubricant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 2640 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID GPR84_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 = 1700 nM (estimated based on the structural similarity with CHEMBL107874 ) [1]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Homo sapiens (Human)
                   UniProt ID GPR84_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 Ki = 2170 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID GPR84_HUMAN
References
1 An Agonist Radioligand for the Proinflammatory Lipid-Activated G Protein-Coupled Receptor GPR84 Providing Structural Insights. J Med Chem. 2020 Mar 12; 63(5):2391-2410.

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