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GoPubMed Proteins lists recent and important papers and reviews for proteins. Page last changed on 08 Dec 2016.

Hydroxycarboxylic acid receptor 1

GPR81, G-protein-coupled receptor 81
G protein-coupled receptors (GPCRs, or GPRs), such as GPR81, contain 7 transmembrane domains and transduce extracellular signals through heterotrimeric G proteins.[supplied by OMIM, Feb 2005] (from NCBI)
Top mentioned proteins: ACID, GPR109A, CAN, V1a, Insulin
Papers on GPR81
Lactate Transport and Receptor Actions in Retina: Potential Roles in Retinal Function and Disease.
New
Bergersen et al., Copenhagen, Denmark. In Neurochem Res, Jan 2016
In the present paper, we argue that the lactate receptor GPR81, also known as HCAR1, may contribute importantly to the control of retinal cell functions in health and disease.
Comprehensive Profiling of GPCR Expression in Ghrelin-producing Cells.
New
Nakao et al., Ōsaka, Japan. In Endocrinology, Jan 2016
Expression levels of GPCRs previously suggested to regulate ghrelin secretion including adrenergic β1 receptor, GPR81, oxytocin receptor, GPR120, and somatostatin receptor 2 were high in MGN3-1 cells.
Synthesis and Pharmacological Properties of Silicon-Containing GPR81 and GPR109A Agonists.
New
Tacke et al., Würzburg, Germany. In Chemmedchem, Dec 2015
The GPR81 and GPR109A receptors mediate antilipolytic effects and are potential drug targets for the treatment of metabolic disorders such as dyslipidemia and type 2 diabetes.
The lactate receptor, G-protein-coupled receptor 81/hydroxycarboxylic acid receptor 1: Expression and action in brain.
Review
New
Bergersen et al., Oslo, Norway. In J Neurosci Res, Jul 2015
We have proposed that lactate is a "volume transmitter" in the brain and underpinned this by showing that the lactate receptor, G-protein-coupled receptor 81 (GPR81, also known as HCA1 or HCAR1), which promotes lipid storage in adipocytes, is also active in the mammalian brain.
Is L-lactate a novel signaling molecule in the brain?
Review
New
Kasparov et al., Bristol, United Kingdom. In J Cereb Blood Flow Metab, Jul 2015
Others postulate interaction with either known receptor HCA1 (GPR81) or a novel, yet unidentified receptor.
Inhibition of G protein-coupled receptor 81 (GPR81) protects against ischemic brain injury.
New
Chen et al., Hangzhou, China. In Cns Neurosci Ther, Mar 2015
G protein-coupled receptor 81 (GPR81) is an endogenous receptor for lactate.
Lactate transport and signaling in the brain: potential therapeutic targets and roles in body-brain interaction.
Review
New
Bergersen, Oslo, Norway. In J Cereb Blood Flow Metab, Feb 2015
Lactate binds to the lactate receptor GPR81 aka hydroxycarboxylic acid receptor (HCAR1) on brain cells and cerebral blood vessels, and regulates the levels of cAMP.
Monocarboxylate transporters in temporal lobe epilepsy: roles of lactate and ketogenic diet.
Review
Bergersen et al., Oslo, Norway. In Brain Struct Funct, 2015
The changes may be an adaptive response aimed at keeping high levels of lactate in the epileptic tissue, which may serve to counteract epileptic activity by downregulating cAMP levels through the lactate receptor GPR81, newly discovered in hippocampus.
Cell surface lactate receptor GPR81 is crucial for cancer cell survival.
Logsdon et al., Houston, United States. In Cancer Res, 2014
GPR81 is a lactate receptor recently identified in adipose and muscle cells that has not been investigated in cancer.
Lactate reduces liver and pancreatic injury in Toll-like receptor- and inflammasome-mediated inflammation via GPR81-mediated suppression of innate immunity.
Mehal et al., West Haven, United States. In Gastroenterology, 2014
We examined whether lactate and the lactate receptor, Gi-protein-coupled receptor 81 (GPR81), regulate TLR induction of signal 1 and limit inflammasome activation and organ injury.
Lactate transport and receptor actions in cerebral malaria.
Bergersen et al., Copenhagen, Denmark. In Front Neurosci, 2013
Lactate binds to the lactate receptor GPR81, recently discovered on brain cells and cerebral blood vessels, causing inhibition of adenylyl cyclase.
International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: recommendations for new pairings with cognate ligands.
Review
Impact
Harmar et al., Cambridge, United Kingdom. In Pharmacol Rev, 2013
The following recommendations are made for new receptor names based on 11 pairings for class A GPCRs: hydroxycarboxylic acid receptors [HCA₁ (GPR81) with lactate, HCA₂ (GPR109A) with 3-hydroxybutyric acid, HCA₃ (GPR109B) with 3-hydroxyoctanoic acid]; lysophosphatidic acid receptors [LPA₄ (GPR23), LPA₅ (GPR92), LPA₆ (P2Y5)]; free fatty acid receptors [FFA4 (GPR120) with omega-3 fatty acids]; chemerin receptor (CMKLR1; ChemR23) with chemerin; CXCR7 (CMKOR1) with chemokines CXCL12 (SDF-1) and CXCL11 (ITAC); succinate receptor (SUCNR1) with succinate; and oxoglutarate receptor [OXGR1 with 2-oxoglutarate].
Identification of Hydroxybenzoic Acids as Selective Lactate Receptor (GPR81) Agonists with Antilipolytic Effects.
Carruthers et al., San Diego, United States. In Acs Med Chem Lett, 2012
Following the characterization of the lactate receptor (GPR81), a focused screening effort afforded 3-hydroxybenzoic acid 1 as a weak agonist of both GPR81 and GPR109a (niacin receptor).
Study of GPR81, the lactate receptor, from distant species identifies residues and motifs critical for GPR81 functions.
GeneRIF
Liu et al., San Diego, United States. In Mol Pharmacol, 2011
demonstrated that the C165-E166-S167-F168 motif at the second extracellular loop is critical for GPR81 function, and the conserved six Cys residues at the extracellular regions are necessary for GPR81 function
International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B).
Review
Impact
IJzerman et al., Bad Nauheim, Germany. In Pharmacol Rev, 2011
The G-protein-coupled receptors GPR81, GPR109A, and GPR109B share significant sequence homology and form a small group of receptors, each of which is encoded by clustered genes.
An autocrine lactate loop mediates insulin-dependent inhibition of lipolysis through GPR81.
Impact
Offermanns et al., Bad Nauheim, Germany. In Cell Metab, 2010
Here we show that lactate activates the G protein-coupled receptor GPR81, which is expressed in adipocytes and mediates antilipolytic effects through G(i)-dependent inhibition of adenylyl cyclase.
Peroxisome proliferator-activated receptor gamma regulates expression of the anti-lipolytic G-protein-coupled receptor 81 (GPR81/Gpr81).
GeneRIF
Kalkhoven et al., Utrecht, Netherlands. In J Biol Chem, 2009
Data show that the coordinated PPARgamma-mediated regulation of the GPR81, GPR109A and GPR109B presents a novel mechanism by which TZDs may reduce circulating free fatty acid levels and perhaps ameliorate insulin resistance in obese patients.
Role of GPR81 in lactate-mediated reduction of adipose lipolysis.
GeneRIF
Waters et al., Rahway, United States. In Biochem Biophys Res Commun, 2009
GPR81 with relatively restricted expression in the adipose tissues functions as a receptor for lactate and can mediate an anti-lipolytic effect of lactate.
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