GPR171

Last updated

GPR171
Identifiers
Aliases GPR171 , H963, G protein-coupled receptor 171
External IDs MGI: 2442043; HomoloGene: 36330; GeneCards: GPR171; OMA:GPR171 - orthologs
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_013308

NM_173398

RefSeq (protein)

NP_037440

NP_775574

Location (UCSC) Chr 3: 151.2 – 151.2 Mb Chr 3: 59 – 59.01 Mb
PubMed search [3] [4]
Wikidata
View/Edit Human View/Edit Mouse

G-protein coupled receptor 171 is a protein that in humans is encoded by the GPR171 gene. [5] [6] It has been recently deorphanised, with its endogenous agonist being a neuropeptide BigLEN which is a cleavage product of ProSAAS. GPR174 has been found to be involved in processes such as pain, anxiety, and appetite regulation, as well as immune system function, and GPR174 agonists may represent a potential target for novel analgesic drugs. Interestingly it seems to show sex-selective signalling, with effects seen in male mice often absent in female mice. [7] [8] [9] [10] [11] [12] [13] [14] [15] [16]

Contents

Ligands

Agonists

References

  1. 1 2 3 GRCh38: Ensembl release 89: ENSG00000174946 Ensembl, May 2017
  2. 1 2 3 GRCm38: Ensembl release 89: ENSMUSG00000050075 Ensembl, May 2017
  3. "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. Jacobs KA, Collins-Racie LA, Colbert M, Duckett M, Golden-Fleet M, Kelleher K, et al. (Dec 1997). "A genetic selection for isolating cDNAs encoding secreted proteins". Gene. 198 (1–2): 289–296. doi:10.1016/S0378-1119(97)00330-2. PMID   9370294.
  6. "Entrez Gene: GPR171 G protein-coupled receptor 171".
  7. Fricker LD, Devi LA (2018). "Orphan neuropeptides and receptors: Novel therapeutic targets". Pharmacology & Therapeutics. 185: 26–33. doi:10.1016/j.pharmthera.2017.11.006. PMC   5899030 . PMID   29174650.
  8. McDermott MV, Afrose L, Gomes I, Devi LA, Bobeck EN (2019). "Opioid-Induced Signaling and Antinociception Are Modulated by the Recently Deorphanized Receptor, GPR171". The Journal of Pharmacology and Experimental Therapeutics. 371 (1): 56–62. doi:10.1124/jpet.119.259242. PMC   6750184 . PMID   31308196.
  9. Ram A, Edwards T, McCarty A, Afrose L, McDermott MV, Bobeck EN (2021). "GPR171 Agonist Reduces Chronic Neuropathic and Inflammatory Pain in Male, but Not Female Mice". Frontiers in Pain Research. 2 695396. Lausanne, Switzerland. doi: 10.3389/fpain.2021.695396 . PMC   8915562 . PMID   35295419.
  10. Fujiwara Y, Torphy RJ, Sun Y, Miller EN, Ho F, Borcherding N, et al. (2021). "The GPR171 pathway suppresses T cell activation and limits antitumor immunity". Nature Communications. 12 (1) 5857. Bibcode:2021NatCo..12.5857F. doi:10.1038/s41467-021-26135-9. PMC   8494883 . PMID   34615877.
  11. Aryal DK, Rodriguiz RM, Nguyen NL, Pease MW, Morgan DJ, Pintar J, et al. (2022). "Mice lacking proSAAS display alterations in emotion, consummatory behavior and circadian entrainment". Genes, Brain and Behavior. 21 (7) e12827. doi:10.1111/gbb.12827. PMC   9444949 . PMID   35878875.
  12. Afrose L, McDermott MV, Bhuiyan AI, Pathak SK, Bobeck EN (2022). "GPR171 activation regulates morphine tolerance but not withdrawal in a test-dependent manner in mice". Behavioural Pharmacology. 33 (7): 442–451. doi:10.1097/FBP.0000000000000692. PMC   9477863 . PMID   35942845.
  13. McDermott MV, Ram A, Mattoon MT, Haderlie EE, Raddatz MC, Thomason MK, et al. (2023). "A small molecule ligand for the novel pain target, GPR171, produces minimal reward in mice". Pharmacology, Biochemistry, and Behavior. 224 173543. doi:10.1016/j.pbb.2023.173543. PMC   11472835 . PMID   36933620.
  14. Fricker LD, Fakira AK, Bobeck EN, Raddatz M, Kim K, Deschepper KD, et al. (2025). "ProSAAS neuropeptides and receptors GPR171 and GPR83: Potential therapeutic applications for pain, anxiety, and body weight regulation". The Journal of Pharmacology and Experimental Therapeutics. 392 (6) 103599. doi:10.1016/j.jpet.2025.103599. PMID   40450835.
  15. Kou F, Li XY, Feng Z, Hua J, Wu X, Gao H, et al. (2025). "GPR171 restrains intestinal inflammation by suppressing FABP5-mediated Th17 cell differentiation and lipid metabolism". Gut. 74 (8): 1279–1292. doi:10.1136/gutjnl-2024-334010. PMID   40074327.
  16. Raddatz MC, Newson CM, Stott M, Campbell C, Bobeck EN (2025). "GPR171 is necessary for normal physiological functions and mood-related behaviors in males, but not females". Behavioural Brain Research. 490 115618. doi:10.1016/j.bbr.2025.115618. PMID   40318809.

Further reading