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GPR171

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From Wikipedia, the free encyclopedia

Protein-coding gene in the species Homo sapiens

GPR171

Identifiers

Aliases

GPR171, H963, G protein-coupled receptor 171

External IDs

MGI:2442043;HomoloGene:36330;GeneCards:GPR171;OMA:GPR171 - orthologs

Gene location (Human)

Chr.	Chromosome 3 (human)^[1]

Band	3q25.1	Start	151,197,832bp^[1]
Band	3q25.1	End	151,203,216bp^[1]

Gene location (Mouse)

Chr.	Chromosome 3 (mouse)^[2]

Band	3\|3 D	Start	59,003,869bp^[2]
Band	3\|3 D	End	59,009,242bp^[2]

RNA expression pattern

Bgee

Human

Mouse (ortholog)

Top expressed in

testicle

buccal mucosa cell

appendix

blood

lymph node

granulocyte

spleen

superficial temporal artery

amniotic fluid

gallbladder

Top expressed in

mesenteric lymph nodes

blood

spleen

thymus

morula

subcutaneous adipose tissue

embryo

embryo

blastocyst

bone marrow

More reference expression data

BioGPS


More reference expression data

Gene ontology
Molecular function	G protein-coupled purinergic nucleotide receptor activity G protein-coupled receptor activity signal transducer activity
Cellular component	integral component of membrane plasma membrane integral component of plasma membrane membrane
Biological process	G protein-coupled receptor signaling pathway negative regulation of myeloid cell differentiation signal transduction G protein-coupled purinergic nucleotide receptor signaling pathway
Sources:Amigo /QuickGO

Orthologs

Species

Human

Mouse

Entrez


29909


229323

Ensembl


ENSG00000174946


ENSMUSG00000050075

UniProt


O14626


Q8BG55

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 aprotein that in humans is encoded by theGPR171gene.^[5]^[6] It has been recently deorphanised, with itsendogenous agonist being aneuropeptide BigLEN which is a cleavage product ofproSAAS. 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 novelanalgesic drugs. 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]

Ligands

[edit]

Agonists

References

[edit]

^^a ^b ^cGRCh38: Ensembl release 89: ENSG00000174946 –Ensembl, May 2017
^^a ^b ^cGRCm38: Ensembl release 89: ENSMUSG00000050075 –Ensembl, May 2017
^"Human PubMed Reference:".National Center for Biotechnology Information, U.S. National Library of Medicine.
^"Mouse PubMed Reference:".National Center for Biotechnology Information, U.S. National Library of Medicine.
^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.
^"Entrez Gene: GPR171 G protein-coupled receptor 171".
^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.
^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.
^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.
^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.
^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.
^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.
^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.
^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.
^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.
^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.

Adams MD, Kerlavage AR, Fleischmann RD, Fuldner RA, Bult CJ, Lee NH, et al. (Sep 1995)."Initial assessment of human gene diversity and expression patterns based upon 83 million nucleotides of cDNA sequence"(PDF).Nature.377 (6547 Suppl):3–174.PMID 7566098.
Joensuu T, Hämäläinen R, Yuan B, Johnson C, Tegelberg S, Gasparini P, et al. (Oct 2001)."Mutations in a novel gene with transmembrane domains underlie Usher syndrome type 3".American Journal of Human Genetics.69 (4):673–684.doi:10.1086/323610.PMC 1226054.PMID 11524702.
Strausberg RL, Feingold EA, Grouse LH, Derge JG, Klausner RD, Collins FS, et al. (Dec 2002)."Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences".Proceedings of the National Academy of Sciences of the United States of America.99 (26):16899–16903.Bibcode:2002PNAS...9916899M.doi:10.1073/pnas.242603899.PMC 139241.PMID 12477932.

Cell surface receptor:G protein-coupled receptors

Class A:Rhodopsin-like

Neurotransmitter

Adrenergic	α1 (A B D) α2 (A B C) β1 β2 β3
Purinergic	Adenosine (A1 A2A A2B A3) P2Y (1 2 4 5 6 8 9 10 11 12 13 14)
Serotonin	(all but5-HT3)5-HT1 (A B D E F) 5-HT2 (A B C) 5-HT (4 5A 6 7)
Other	Acetylcholine (M1 M2 M3 M4 M5) Dopamine D1 D2 D3 D4 D5 GHB receptor Histamine H1 H2 H3 H4 Melatonin (1A 1B 1C) TAAR (1 2 5 6 8 9)

Metabolites and
signaling molecules

Eicosanoid	CysLT (1 2) LTB4 1 2 FPRL1 OXE Prostaglandin DP (1 2),EP (1 2 3 4),FP Prostacyclin Thromboxane
Other	Bile acid Cannabinoid (CB1 CB2,GPR (18 55 119)) EBI2 Estrogen Free fatty acid (1 2 3 4) Hydroxycarboxylic acids 1 2 3 Lysophosphatidic acid (1 2 3 4 5 6) Lysophospholipid (1 2 3 4 5 6 7 8) Oxoglutarate PAF Sphingosine-1-phosphate (1 2 3 4 5) Succinate

Peptide

Neuropeptide

B/W (1
2)
FF (1
2)
S
Y (1
2
4
5)
Neuromedin (B
U (1
2))
Neurotensin (1
2)

Other

Anaphylatoxin (C3a
C5a (1
2))
Angiotensin (1
2)
Apelin
Bombesin
- BRS3
- GRPR
- NMBR)
- Bradykinin (B1
- B2)
Chemerin
- 1
- 2
Chemokine
Cholecystokinin (A
B)
Endothelin
- A
- B
Formyl peptide (1
2
3)
FSH
Galanin (1
2
3)
Gonadotropin-releasing hormone (1
2)
Ghrelin
Kisspeptin
Luteinizing hormone/choriogonadotropin
MAS (1
1L
D
E
F
G
X1
X2
X3
X4)
Melanocortin (1
2
3
4
5)
MCHR (1
2)
Motilin
Opioid (Delta
Kappa
Mu
Nociceptin &Zeta, but notSigma)
Orexin (1
2)
Oxytocin
Prokineticin (1
2)
Prolactin-releasing peptide
Relaxin (1
2
3
4)
Somatostatin (1
2
3
4
5)
Tachykinin (1
2
3)
Thyrotropin
Thyrotropin-releasing hormone
Urotensin-II
Vasopressin (1A
1B
2)

Miscellaneous

Taste, bitter	TAS2R 1 3 4 5 7 8 9 10 13 14 16 19 20 30 31 38 39 40 41 42 43 45 46 50 60 Vomeronasal receptor type 1
Orphan	GPR (3 4 6 12 15 17 18 19 20 21 22 26 27 31 32 33 34 35 37 39 42 45 50 52 55 61 62 63 65 68 75 78 82 83 84 85 87 88 101 103 109A 119 132 135 137B 139 141 142 146 148 149 150 151 152 153 160 161 162 171 173 174 176 177 182 183)
Other	Adrenomedullin Olfactory Opsin (3 4 5 1LW 1MW 1SW RGR RRH) Protease-activated (1 2 3 4) SREB (1 2 3)

Class B:Secretin-like

Adhesion	ADGRB Brain-specific angiogenesis inhibitor 1 2 3 ADGRC Cadherin 1 2 3 ADGRE EMR 1 2 3 CD97 ADGRG 1 2 3 4 5 6 7 ADGRL Latrophilin 1 2 3 ELTD1
Orphan	GPR (56 64 97 98 110 111 112 113 114 115 116 123 124 125 126 128 133 143 144 155 157)
Other	Calcitonin CALCRL Corticotropin-releasing hormone (1 2) Glucagon (GR GIPR GLP1R GLP2R) Growth-hormone-releasing hormone PACAPR1 GPR Methuselah-like proteins Parathyroid hormone (1 2) Secretin Vasoactive intestinal peptide (1 2)

Class C:Metabotropic glutamate /pheromone

Taste, sweet	TAS1R 1 2 3 Vomeronasal receptor, type 2
Other	Calcium-sensing receptor GABA_B (1 2) Glutamate receptor (Metabotropic glutamate (1 2 3 4 5 6 7 8)) GPRC6A GPR (156 158 179) RAIG (1 2 3 4)

Class F:Frizzled &Smoothened

Frizzled	Frizzled (1 2 3 4 5 6 7 8 9 10)
Smoothened	Smoothened

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