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Hydroxycarboxylic acid receptor 1

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(Redirected fromGPR81)
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
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
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
PubMedsearch[3][4]
Wikidata
View/Edit HumanView/Edit Mouse

Hydroxycarboxylic acid receptor 1(HCA1), formerly known asG protein-coupled receptor 81(GPR81), is aproteinthat in humans is encoded by theHCAR1gene.[5][6]HCA1,like the otherhydroxycarboxylic acid receptorsHCA2andHCA3,is aGi/o-coupledG protein-coupled receptor(GPCR).[7][8]The primaryendogenousagonistof HCA1islactic acid(and itsconjugate base,lactate).[7][8]More recently,3,5-dihydroxybenzoic acidhas been reported to activate HCA1.[9]

Lactatewas initially found to activate HCA1onfat cellsand thereby to inhibit these cellslipolysisi.e., break-down of their fats intofree fatty acidsandglycerol.[10][11]Subsequent studies have found that in addition to fat cells, HCA1is expressed on cells in the brain, skeletal muscle, lymphoid tissue, uterus, kidney, liver, and pancreas as well as on immune cells such asmacrophagesandantigen-presenting cells.In the brain, HCA1acts to dampenneuronexcitation and may also function to promoteneurogenesis(i.e., production of neurons fromneural stem cells) andangiogenesis,i.e., formation of new blood vessels from pre-existing blood vessels). The functions of HCA1in 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]

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, Lewis T, Evans JF, George SR, O'Dowd BF (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.PMID11574155.
  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.PMID21454438.
  8. ^abS Offermanns, SL Colletti, AP IJzerman, TW Lovenberg, G Semple, A Wise, MG Waters."Hydroxycarboxylic acid receptors".IUPHAR/BPS Guide to Pharmacology.International Union of Basic and Clinical Pharmacology.Retrieved13 July2018.{{cite web}}:CS1 maint: multiple names: authors list (link)
  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:1–19.doi:10.1080/10408398.2023.2203762.PMID37096487.S2CID258310985.
  10. ^Liu C, Wu J, Zhu J, Kuei C, Yu J, Shelton J, Sutton SW, Li X, Yun SJ, Mirzadegan T, Mazur C, Kamme F, Lovenberg TW (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.PMID19047060.
  11. ^Cai TQ, Ren N, Jin L, Cheng K, Kash S, Chen R, Wright SD, Taggart AK, Waters MG (December 2008). "Role of GPR81 in lactate-mediated reduction of adipose lipolysis".Biochemical and Biophysical Research Communications.377(3): 987–91.doi:10.1016/j.bbrc.2008.10.088.PMID18952058.
  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.PMID37391123.S2CID259279124.

Further reading[edit]