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GPR32

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Target not currently curated in GtoImmuPdb

Target id: 99

Nomenclature: GPR32

Family: Class A Orphans with emerging pharmacology

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 356 19q13.33 GPR32 G protein-coupled receptor 32
Previous and Unofficial Names Click here for help
RvD1 | RVDR1 | resolvin D1 receptor
Database Links Click here for help
Specialist databases
GPCRdb gpr32_human (Hs)
Other databases
Alphafold O75388 (Hs)
ChEMBL Target CHEMBL4523863 (Hs)
Ensembl Gene ENSG00000142511 (Hs)
Entrez Gene 2854 (Hs)
Human Protein Atlas ENSG00000142511 (Hs)
KEGG Gene hsa:2854 (Hs)
OMIM 603195 (Hs)
Pharos O75388 (Hs)
RefSeq Nucleotide NM_001506 (Hs)
RefSeq Protein NP_001497 (Hs)
UniProtKB O75388 (Hs)
Wikipedia GPR32 (Hs)
Natural/Endogenous Ligands Click here for help
LXA4
resolvin D1
Comments: Proposed ligand, single publication
Potency order of endogenous ligands
resolvin D1 > LXA4

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]resolvin D1 Small molecule or natural product Ligand is labelled Ligand is radioactive Immunopharmacology Ligand Hs Agonist 9.7 pKd 3
⤷ pKd 9.7 (Kd 2x10-10 M) [3]
RvD1-ME Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Full agonist 11.3 pEC50 2
⤷ pEC50 11.3 (EC50 4.6x10-12 M) [2]
resolvin D1 Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 11.1 pEC50 3
⤷ pEC50 11.1 (EC50 8.8x10-12 M) [3]
LXA4 Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 9.7 pEC50 3
⤷ pEC50 9.7 (EC50 2x10-10 M) [3]
Agonist Comments
Resolvin D1 has been demonstrated to activate GPR32 in a single publication [3]. This result is supported by the findings of Chiang et al. which demonstrate that Resolvin D1 inhibits TNFalpha mediated NFκB activation via GPR32 [1]. The pairing was not replicated in a recent studty based on β-arrestin recruitment [6].
Immuno Process Associations
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 2 GO processes
GO:0002430 complement receptor mediated signaling pathway IBA
GO:0004875 complement receptor activity IBA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 2 GO processes
GO:0002430 complement receptor mediated signaling pathway IBA
GO:0004875 complement receptor activity IBA
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes
GO:0006954 inflammatory response IBA
Tissue Distribution Click here for help
Arterial and venous tissue
Species:  Human
Technique:  Microarray analysis
References:  3
Myeloid cells, human umbilical vein cells
Species:  Human
Technique:  RT-PCR
References:  3
Tissue Distribution Comments
Surface expression in human monocytes up-regulated by zymosan and G-CSF [3].
Physiological Consequences of Altering Gene Expression Click here for help
Overexpression of GPR32 enhances RvD1 mediated macrophage phagocytosis of human polymorphonuclear leukocytes
Species:  Human
Tissue:  Macrophage
Technique:  RNA interference
References:  3
Selective knockdown decreases RvD1 mediate macrophage phagocytosis of human polymorphonuclear leukocytes
Species:  Human
Tissue:  Macrophage
Technique:  RNA interference
References:  3
Macrophages overexpressing GPR32 show significantly upregulated miRNA-21, and downregulation of miR-302d and miR-219
Species:  Mouse
Tissue:  Macrophage
Technique:  Gene overexpression
References:  5
Biologically Significant Variants Click here for help
Type:  Single nucleotide polymorphism
Species:  Human
Amino acid change:  F327L
Global MAF (%):  2
Subpopulation MAF (%):  AMR|ASN|EUR: 3|2|3
Minor allele count:  C=0.021/47
Comment on frequency:  Low frequency (<10% in all tested populations)
SNP accession:  VAR_011860, rs1864011
Validation:  1000 Genomes, Frequency
Type:  Single nucleotide polymorphism
Species:  Human
Amino acid change:  P354S
Global MAF (%):  1
Subpopulation MAF (%):  AFR: 2
Minor allele count:  T=0.005/11
Comment on frequency:  Low frequency (<10% in all tested populations)
SNP accession:  rs75959054
Validation:  Frequency
General Comments
GPR32 is a pseudogene in mice and rats [3].

Resolvin mediated activation of GPR32 may be important in the resolution of inflammatory disease [4].

References

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1. Chiang N, Fredman G, Bäckhed F, Oh SF, Vickery T, Schmidt BA, Serhan CN. (2012) Infection regulates pro-resolving mediators that lower antibiotic requirements. Nature, 484 (7395): 524-8. [PMID:22538616]

2. Krishnamoorthy S, Recchiuti A, Chiang N, Fredman G, Serhan CN. (2012) Resolvin D1 receptor stereoselectivity and regulation of inflammation and proresolving microRNAs. Am J Pathol, 180 (5): 2018-27. [PMID:22449948]

3. Krishnamoorthy S, Recchiuti A, Chiang N, Yacoubian S, Lee CH, Yang R, Petasis NA, Serhan CN. (2010) Resolvin D1 binds human phagocytes with evidence for proresolving receptors. Proc Natl Acad Sci USA, 107 (4): 1660-5. [PMID:20080636]

4. Lee CH. (2012) Resolvins as new fascinating drug candidates for inflammatory diseases. Arch Pharm Res, 35 (1): 3-7. [PMID:22297737]

5. Pappo AS, Krailo M, Chen Z, Rodriguez-Galindo C, Reaman G. (2010) Infrequent tumor initiative of the Children's Oncology Group: initial lessons learned and their impact on future plans. J Clin Oncol, 28 (33): 5011-6. [PMID:20956621]

6. Southern C, Cook JM, Neetoo-Isseljee Z, Taylor DL, Kettleborough CA, Merritt A, Bassoni DL, Raab WJ, Quinn E, Wehrman TS et al.. (2013) Screening β-Arrestin Recruitment for the Identification of Natural Ligands for Orphan G-Protein-Coupled Receptors. J Biomol Screen, 18 (5): 599-609. [PMID:23396314]

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