GPR81

HCAR1

Identifiers

HCAR1, GPR104, GPR81, HCA1, LACR1, TA-GPCR, TAGPCR, FKSG80, hydroxycarboxylic acid receptor 1

External IDs

MGI: 2441671 HomoloGene: 13060 GeneCards: HCAR1

Targeted by Drug

niacin, 3,5-dihydroxybenzoic acid, 4-hydroxybutanoic acid^[1]

Gene ontology
Molecular function	• G-protein coupled receptor activity • signal transducer activity
Cellular component	• integral component of membrane • plasma membrane • membrane
Biological process	• G-protein coupled receptor signaling pathway • xenophagy • signal transduction • positive regulation of defense response to virus by host
Sources:Amigo / QuickGO

RNA expression pattern

More reference expression data

Orthologs

Species

Human

Mouse

Entrez


27198


243270

Ensembl


ENSG00000196917


ENSMUSG00000049241

UniProt


Q9BXC0


Q8C131

RefSeq (mRNA)


NM_032554


NM_175520

RefSeq (protein)


NP_115943.1


n/a

Location (UCSC)

Chr 12: 122.73 – 122.73 Mb

Chr 5: 123.88 – 123.88 Mb

PubMed search

^[2]

^[3]

Wikidata

View/Edit Human

View/Edit Mouse

G protein-coupled receptor 81, also known as GPR81, is a protein that in humans is encoded by the GPR81 gene.^[4]^[5]

G protein-coupled receptors (GPCRs, or GPRs), such as GPR81, contain 7 transmembrane domains and transduce extracellular signals through heterotrimeric G proteins.^[4]

Lactate activates the GPR81 receptor which in turn inhibits lipolysis in fat cells.^[6]^[7]

References

↑ "Drugs that physically interact with Hydroxycarboxylic acid receptor 1 view/edit references on wikidata".
↑ "Human PubMed Reference:".
↑ "Mouse PubMed Reference:".
1 2 "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.
↑ 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.

Takeda S, Kadowaki S, Haga T, Takaesu H, Mitaku S (June 2002). "Identification of G protein-coupled receptor genes from the human genome sequence". FEBS Letters. 520 (1-3): 97–101. doi:10.1016/S0014-5793(02)02775-8. PMID 12044878.
Mao M, Biery MC, Kobayashi SV, Ward T, Schimmack G, Burchard J, Schelter JM, Dai H, He YD, Linsley PS (June 2004). "T lymphocyte activation gene identification by coregulated expression on DNA microarrays". Genomics. 83 (6): 989–99. doi:10.1016/j.ygeno.2003.12.019. PMID 15177553.
Madaan A, Nadeau-Vallée M, Rivera JC, Obari D, Hou X, Sierra EM, Girard S, Olson DM, Chemtob S (September 2016). "Lactate produced during labor modulates uterine inflammation via GPR81 (HCA1)". American Journal of Obstetrics and Gynecology. doi:10.1016/j.ajog.2016.09.072. PMID 27615440.

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 but 5-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) Histamine (H1 H2 H3 H4) Melatonin (1A 1B 1C) TAAR (1 2 3 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) Lactate Lysophosphatidic acid (1 2 3 4 5 6) Lysophospholipid (1 2 3 4 5 6 7 8) Niacin (1 2) 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) Angiotensin (1 2) Apelin Bombesin (BRS3 GRPR NMBR) Bradykinin (B1 B2) Chemokine Cholecystokinin (A B) Endothelin (A B) Formyl peptide (1 2 3) FSH Galanin (1 2 3) GHB receptor 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 not Sigma) 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

Orphan	GPR (1 3 4 6 12 15 17 18 19 20 21 22 23 25 26 27 31 32 33 34 35 37 39 42 44 45 50 52 55 61 62 63 65 68 75 77 78 81 82 83 84 85 87 88 92 101 103 109A 109B 119 120 132 135 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	ADGRG (1 2 3 4 5 6 7)

Orphan	GPR (56 64 97 98 110 111 112 113 114 115 116 123 124 125 126 128 133 143 144 155 157)

Other	Brain-specific angiogenesis inhibitor (1 2 3) Cadherin (1 2 3) Calcitonin CALCRL CD97 Corticotropin-releasing hormone (1 2) EMR (1 2 3) Glucagon (GR GIPR GLP1R GLP2R) Growth hormone releasing hormone PACAPR1 GPR Latrophilin (1 2 3 ELTD1) Methuselah-like proteins Parathyroid hormone (1 2) Secretin Vasoactive intestinal peptide (1 2)

Class C: Metabotropic glutamate / pheromone

Taste	TAS1R (1 2 3) 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)

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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GPR81

References

Further reading