dentate gyrus of hippocampal formation granule cell
right kidney
lacrimal gland
More reference expression data
BioGPS
More reference expression data
Gene ontology
Molecular function
G protein-coupled receptor activity
signal transducer activity
Cellular component
integral component of membrane
plasma membrane
membrane
Biological process
signal transduction
G protein-coupled receptor signaling pathway
Sources:Amigo / QuickGO
Orthologs
Species
Human
Mouse
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 Mb
Chr 5: 124.01 – 124.02 Mb
PubMed search
[3]
[4]
Wikidata
View/Edit Human
View/Edit Mouse
Hydroxycarboxylic acid receptor 1 (HCA1), formerly known as G protein-coupled receptor 81 (GPR81), is a protein that in humans is encoded by the HCAR1 gene.[5][6] HCA1, like the other hydroxycarboxylic acid receptors HCA2 and HCA3, is a Gi/o-coupled G protein-coupled receptor (GPCR).[7][8] The primary endogenous agonist of HCA1 is lactic acid (and its conjugate base, lactate).[7][8] More recently, 3,5-dihydroxybenzoic acid has been reported to activate HCA1.[9]
Lactate was initially found to activate HCA1 on fat cells and thereby to inhibit these cells lipolysis i.e., break-down of their fats into free fatty acids and glycerol.[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 as macrophages and antigen-presenting cells. In the brain, HCA1 acts to dampen neuron excitation and may also function to promote neurogenesis (i.e., production of neurons from neural stem cells) and angiogenesis, i.e., 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]
^ abcGRCh38: Ensembl release 89: ENSG00000196917 – Ensembl, May 2017
^ abcGRCm38: Ensembl release 89: ENSMUSG00000049241 – 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.
^"Entrez Gene: GPR81 G protein-coupled receptor 81".
^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. PMID 11574155.
^ 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.
^ 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. Retrieved 13 July 2018.{{cite web}}: CS1 maint: multiple names: authors list (link)
^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. PMID 37096487. S2CID 258310985.
^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. PMID 19047060.
^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. PMID 18952058.
^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.
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from a common ancestral receptor. In fact, relatively minor mutations, such as a change in 3 amino acids in many of these receptors can convert a cation-selective...
are a subclass of hydroxycarboxylicacids. The C16 and C18 omega hydroxy acids 16-hydroxy palmitic acid and 18-hydroxy stearic acid are key monomers of...
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