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Hydroxycarboxylic acid receptor 1

From Wikipedia, the free encyclopedia
Protein-coding gene in the species Homo sapiens

HCAR1
Identifiers
AliasesHCAR1, GPR104, GPR81, HCA1, LACR1, TA-GPCR, TAGPCR, FKSG80, hydroxycarboxylic acid receptor 1
External IDsOMIM:606923;MGI:2441671;HomoloGene:13060;GeneCards:HCAR1;OMA:HCAR1 - orthologs
Gene location (Human)
Chromosome 12 (human)
Chr.Chromosome 12 (human)[1]
Chromosome 12 (human)
Genomic location for HCAR1
Genomic location for HCAR1
Band12q24.31Start122,726,076bp[1]
End122,730,844bp[1]
Gene location (Mouse)
Chromosome 5 (mouse)
Chr.Chromosome 5 (mouse)[2]
Chromosome 5 (mouse)
Genomic location for HCAR1
Genomic location for HCAR1
Band5|5 FStart124,014,799bp[2]
End124,018,083bp[2]
RNA expression pattern
Bgee
HumanMouse (ortholog)
Top expressed in
  • gonad

  • spleen

  • minor salivary glands

  • body of stomach

  • subcutaneous adipose tissue

  • stromal cell of endometrium

  • right lobe of thyroid gland

  • left lobe of thyroid gland

  • ganglionic eminence

  • human kidney
Top expressed in
  • brown adipose tissue

  • white adipose tissue

  • mammary gland

  • embryo

  • transitional epithelium of urinary bladder

  • subcutaneous adipose tissue

  • esophagus

  • dentate gyrus of hippocampal formation granule cell

  • right kidney

  • lacrimal gland
More reference expression data
BioGPS
More reference expression data
Gene ontology
Molecular function
Cellular component
Biological process
Sources:Amigo /QuickGO
Orthologs
SpeciesHumanMouse
Entrez

27198

243270

Ensembl

ENSG00000196917

ENSMUSG00000049241

UniProt

Q9BXC0

Q8C131

RefSeq (mRNA)

NM_032554

NM_175520

RefSeq (protein)

NP_115943

NP_780729

Location (UCSC)Chr 12: 122.73 – 122.73 MbChr 5: 124.01 – 124.02 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/Edit Mouse

Hydroxycarboxylic acid receptor 1 (HCA1), formerly known asG protein-coupled receptor 81 (GPR81), is aprotein that in humans is encoded by theHCAR1gene.[5][6] HCA1, like the otherhydroxycarboxylic acid receptorsHCA2 andHCA3, is aGi/o-coupledG protein-coupled receptor (GPCR).[7][8] The primaryendogenousagonist of HCA1 islactic acid (and itsconjugate base, lactate).[7][8] More recently,3,5-dihydroxybenzoic acid has been reported to activate HCA1.[9]

Lactate was initially found to activate HCA1 onfat cells and thereby to inhibit these cellslipolysis i.e., break-down of their fats intofree fatty acids andglycerol.[10][11] Subsequent studies have found that in addition to fat cells, HCA1 is expressed on cells in the brain, skeletal muscle, lymphoid tissue, uterus, kidney, liver, and pancreas as well as on immune cells such asmacrophages andantigen-presenting cells. In the brain, HCA1 acts to dampenneuron excitation and may also function to promoteneurogenesis (the production of neurons fromneural stem cells) andangiogenesis (the formation of new blood vessels from pre-existing blood vessels). The functions of HCA1 in non-fat and non-neural tissues have not been fully defined but in many cases appear to involve promoting the survival of cells, including various types of cancer cells.[12]

Ligands

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Agonists

References

[edit]
  1. ^abcGRCh38: Ensembl release 89: ENSG00000196917Ensembl, May 2017
  2. ^abcGRCm38: Ensembl release 89: ENSMUSG00000049241Ensembl, 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. ^"Entrez Gene: GPR81 G protein-coupled receptor 81".
  6. ^Lee DK, Nguyen T, Lynch KR, Cheng R, Vanti WB, Arkhitko O, et al. (September 2001). "Discovery and mapping of ten novel G protein-coupled receptor genes".Gene.275 (1):83–91.doi:10.1016/S0378-1119(01)00651-5.PMID 11574155.
  7. ^abOffermanns S, Colletti SL, Lovenberg TW, Semple G, Wise A, IJzerman AP (June 2011)."International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B)".Pharmacological Reviews.63 (2):269–90.doi:10.1124/pr.110.003301.PMID 21454438.
  8. ^abOffermanns S, Colletti SL, IJzerman AP, Lovenberg TW, Semple G, Wise A, et al."Hydroxycarboxylic acid receptors".IUPHAR/BPS Guide to Pharmacology. International Union of Basic and Clinical Pharmacology. Retrieved13 July 2018.
  9. ^Wagner W, Sobierajska K, Pułaski Ł, Stasiak A, Ciszewski WM (April 2023). "Whole grain metabolite 3,5-dihydroxybenzoic acid is a beneficial nutritional molecule with the feature of a double-edged sword in human health: a critical review and dietary considerations".Critical Reviews in Food Science and Nutrition.64 (24):8786–8804.doi:10.1080/10408398.2023.2203762.PMID 37096487.S2CID 258310985.
  10. ^Liu C, Wu J, Zhu J, Kuei C, Yu J, Shelton J, et al. (January 2009)."Lactate inhibits lipolysis in fat cells through activation of an orphan G-protein-coupled receptor, GPR81".The Journal of Biological Chemistry.284 (5):2811–22.doi:10.1074/jbc.M806409200.PMID 19047060.
  11. ^Cai TQ, Ren N, Jin L, Cheng K, Kash S, Chen R, et al. (December 2008). "Role of GPR81 in lactate-mediated reduction of adipose lipolysis".Biochemical and Biophysical Research Communications.377 (3):987–91.Bibcode:2008BBRC..377..987C.doi:10.1016/j.bbrc.2008.10.088.PMID 18952058.
  12. ^Colucci AC, Tassinari ID, Loss ED, de Fraga LS (June 2023). "History and Function of the Lactate Receptor GPR81/HCAR1 in the Brain: A Putative Therapeutic Target for the Treatment of Cerebral Ischemia".Neuroscience.526:144–163.doi:10.1016/j.neuroscience.2023.06.022.PMID 37391123.S2CID 259279124.
  13. ^Jones NK, Stewart K, Czopek A, Menzies RI, Thomson A, Moran CM, et al. (May 2020)."Endothelin-1 Mediates the Systemic and Renal Hemodynamic Effects of GPR81 Activation".Hypertension.75 (5):1213–1222.doi:10.1161/HYPERTENSIONAHA.119.14308.PMC 7176350.PMID 32200679.

Further reading

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