General Information of Target

Target ID LDTP12431
Target Name G-protein coupled receptor 84 (GPR84)
Gene Name GPR84
Gene ID 53831
Synonyms
EX33; G-protein coupled receptor 84; Inflammation-related G-protein coupled receptor EX33
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MARTLRPSPLCPGGGKAQLSSASLLGAGLLLQPPTPPPLLLLLFPLLLFSRLCGALAGPI
IVEPHVTAVWGKNVSLKCLIEVNETITQISWEKIHGKSSQTVAVHHPQYGFSVQGEYQGR
VLFKNYSLNDATITLHNIGFSDSGKYICKAVTFPLGNAQSSTTVTVLVEPTVSLIKGPDS
LIDGGNETVAAICIAATGKPVAHIDWEGDLGEMESTTTSFPNETATIISQYKLFPTRFAR
GRRITCVVKHPALEKDIRYSFILDIQYAPEVSVTGYDGNWFVGRKGVNLKCNADANPPPF
KSVWSRLDGQWPDGLLASDNTLHFVHPLTFNYSGVYICKVTNSLGQRSDQKVIYISDPPT
TTTLQPTIQWHPSTADIEDLATEPKKLPFPLSTLATIKDDTIATIIASVVGGALFIVLVS
VLAGIFCYRRRRTFRGDYFAKNYIPPSDMQKESQIDVLQQDELDSYPDSVKKENKNPVNN
LIRKDYLEEPEKTQWNNVENLNRFERPMDYYEDLKMGMKFVSDEHYDENEDDLVSHVDGS
VISRREWYV
Target Type
Clinical trial
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family
Subcellular location
Cell membrane
Function
G protein-coupled receptor that responds endogenously to dietary fatty acids or nutrient, specifically 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. In immune cells, functions as a pro-inflammatory receptor via 6-OAU and promotes the expression of pro-inflammatory mediators such as TNFalpha, IL-6 and IL-12B as well as stimulating chemotactic responses through activation of signaling mediators AKT, ERK and NF-kappa-B. In addition, triggers increased bacterial adhesion and phagocytosis in macrophages and regulates pro-inflammatory function via enhancing NLRP3 inflammasome activation. Plays also an important role in inflammation by modulating neutrophil functions. Mechanistically, promotes neutrophil chemotaxis, reactive oxygen species (ROS) production and degranulation via LYN-AKT/ERK pathway. To regulate ROS, communicates with the two formyl peptide receptors FPR2 and FPR1 to control the NADPH oxidase activity in neutrophils.
TTD ID
T98091
Uniprot ID
Q9NQS5
DrugMap ID
TTG0MQD
Ensemble ID
ENST00000267015.4
HGNC ID
HGNC:4535
ChEMBL ID
CHEMBL3714079

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Acrolein
 Probe Info 
N.A.  LDD0223  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0109  NEM HeLa N.A.  LDD0223  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pbi-4050 Small molecular drug DT56YX
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Shr0534 . DZLM72
Investigative
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
2-hydroxy Capric Acid Small molecular drug D0E1UA
2-hydroxylauric Acid Small molecular drug D0T4BP
3-hydroxy Capric Acid Small molecular drug D03GHN
3-hydroxylauric Acid Small molecular drug D0T2CG
6-n-octylaminouracil Small molecular drug D0R1MM
Undecanoic Acid Small molecular drug D0X0PF

References

1 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.