Property Summary

NCBI Gene PubMed Count 40
PubMed Score 119.20
PubTator Score 98.90

Knowledge Summary

Patent (18,477)

Gene RIF (32)

26656756 new insights into the G protein coupling profiles of the HCA receptors and the function of the receptor's C terminus
25690651 Results suggest that the atypical motif asparaging-cysteine-systeine Asn(17)-Cys(18)-Cys(19) is crucial for the normal surface trafficking and function of hydroxycarboxylic acid receptor 2 protein hGPR109A.
25463108 niacin, at a relatively low concentration, preserves the ability of HMVEC to form tubes under conditions of saturated fatty acid excess, and may elicit this effect through activation of GPR109A
25375133 These results suggest that the PKC pathway and PDGFR/EGFR transactivation pathway play important roles in HCA2-mediated Akt activation.
25361930 The results of this study suggested that GPR109A signaling is associated with T2DM, playing a role in regulation of the inflammatory cytokines.
25329911 GPR109A expression is upregulated in blood and substantia nigra in Parkinson disease patients.
24662263 the promiscuous activity exerted by niacin via both GPR109A and GPER may open new avenues towards a better understanding of the mechanisms involved in its biological action exerted in different pathophysiological conditions, including malignant diseases.
24371223 GPR109A is a tumor suppressor in mammary gland.
24215154 Although its functional role is still unknown, HCA2 may be potentially involved in the pathogenesis of various retinopathies and may offer a new therapeutic target.
23770183 These studies provide key insights into mechanisms by which GPR109A may influence cholesterol efflux in macrophages.
23658787 despite NA's anti-inflammatory effect on human macrophages, it has no effect on foam cells in reverse cholesterol transport; due to GPR109A down-regulation
23526298 Review of the role of GPR109A and its downstream effects in the context of atherosclerosis and vascular inflammation, along with insights into strategy for future drug development. [Review Article]
22962331 A sequence from residues 329 to 343 in the C-terminal tail of HCA plays a crucial role in keeping HCA in an inactive conformation.
22267479 Nicotnic acid displays a range of effects that are lipoprotein-independent and potentially antiatherogenic. These effects are mediated by GPR109A.
21768093 upon binding to niacin GPR109A receptors initially activate G(i), leading to dissociation of the Gbetagamma subunit from activated G(i), and subsequently induce ERK1/2 activation via two distinct pathways.
21655214 In contrast, in a squamous cell carcinoma derived cell line, both GPR109A and GPR109B show a more diffuse cellular localization and the receptors are nearly non-functional.
20655299 niacin-mediated activation of GP109A in liver lowers ABCA1 expression leading to reduced hepatic cholesterol efflux to high density lipoprotein.
20628086 Observational study of gene-disease association, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator)
20460384 The agonist-induced internalization of GPR109A receptors is regulated by GRK2 and arrestin3 in a pertussis toxin-sensitive manner and that internalized receptor recycling is independent of endosomal acidification.
20380810 these results demonstrate that GPR109A and GPR109B dimerization is a constitutive process occurring early during biosynthesis.
20184326 Data show that Mk-6892 was discovered as full and potent niacin receptor (GPR109A) agonist.
19913121 Observational study of gene-disease association. (HuGE Navigator)
19633298 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.
19502010 Observational study of gene-disease association and gene-gene interaction. (HuGE Navigator)
19141678 GPR109A receptor plays an important role in the dual regulation of adiponectin secretion and lipolysis
19136666 Data show that many phenolic acids, including those from the hydroxybenzoic and hydroxycinnamic acid classes, can bind and activate GPR109A (HM74a/PUMA-G), the receptor for the antidyslipidemic agent nicotinic acid.
18787507 Observational study of gene-disease association. (HuGE Navigator)
18639743 Data show that the high-affinity niacin receptor HM74A is significantly down-regulated in the anterior cingulate cortex of individuals with schizophrenia.
17932499 neutrophils express functional GPR109A receptors,which might be involved in the regulation of neutrophil numbers
16674924 However, the synergistic effects of HM74A were not dramatically affected by co-treatment with both inhibitors, indicating the cross-talk occurred at the receptor level.
16018973 Our results provided direct evidence indicating that HM74A, but not HM74, was sufficient to mediate anti-lipolytic effect of niacin in adipose tissue.
12646212 HM74b has high similarity to HM74 is a receptor for nicotinic acid [HM74b]

AA Sequence

EPWSPSYLGPTSP                                                             351 - 363

Text Mined References (40)

PMID Year Title
26656756 2016 The role of the C-terminus of the human hydroxycarboxylic acid receptors 2 and 3 in G protein activation using G?-engineered yeast cells.
25690651 2015 The atypical N-glycosylation motif, Asn-Cys-Cys, in human GPR109A is required for normal cell surface expression and intracellular signaling.
25463108 2014 Niacin receptor activation improves human microvascular endothelial cell angiogenic function during lipotoxicity.
25375133 2014 Niacin activates the PI3K/Akt cascade via PKC- and EGFR-transactivation-dependent pathways through hydroxyl-carboxylic acid receptor 2.
25361930 2014 The expression of GPR109A, NF-kB and IL-1? in peripheral blood leukocytes from patients with type 2 diabetes.
25329911 2014 Upregulation of GPR109A in Parkinson's disease.
24662263 2014 Niacin activates the G protein estrogen receptor (GPER)-mediated signalling.
24371223 2014 The niacin/butyrate receptor GPR109A suppresses mammary tumorigenesis by inhibiting cell survival.
24215154 2014 Constitutive expression of HCA(2) in human retina and primary human retinal pigment epithelial cells.
23770183 2013 Differential tissue and ligand-dependent signaling of GPR109A receptor: implications for anti-atherosclerotic therapeutic potential.
23658787 2013 Nicotinic acid receptor GPR109A is down-regulated in human macrophage-derived foam cells.
23526298 2013 GPR109A and vascular inflammation.
22962331 2012 Identification and characterization of distinct C-terminal domains of the human hydroxycarboxylic acid receptor-2 that are essential for receptor export, constitutive activity, desensitization, and internalization.
22267479 2012 Anti-inflammatory effects of nicotinic acid in human monocytes are mediated by GPR109A dependent mechanisms.
21768093 2011 Distinct kinetic and spatial patterns of protein kinase C (PKC)- and epidermal growth factor receptor (EGFR)-dependent activation of extracellular signal-regulated kinases 1 and 2 by human nicotinic acid receptor GPR109A.
21655214 2011 Nicotinic acid receptor abnormalities in human skin cancer: implications for a role in epidermal differentiation.
21454438 2011 International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B).
21167710 2011 Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A).
20655299 2010 Modulation of HDL metabolism by the niacin receptor GPR109A in mouse hepatocytes.
20628086 2010 Variation at the NFATC2 locus increases the risk of thiazolidinedione-induced edema in the Diabetes REduction Assessment with ramipril and rosiglitazone Medication (DREAM) study.
20460384 2010 Internalization of the human nicotinic acid receptor GPR109A is regulated by G(i), GRK2, and arrestin3.
20380810 2010 Evidence for constitutive dimerization of niacin receptor subtypes.
20184326 2010 Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.
19913121 2009 Gene-centric association signals for lipids and apolipoproteins identified via the HumanCVD BeadChip.
19633298 2009 Peroxisome proliferator-activated receptor gamma regulates expression of the anti-lipolytic G-protein-coupled receptor 81 (GPR81/Gpr81).
19502010 2009 Two complex genotypes relevant to the kynurenine pathway and melanotropin function show association with schizophrenia and bipolar disorder.
19141678 2009 Niacin stimulates adiponectin secretion through the GPR109A receptor.
19136666 2009 Phenolic acids suppress adipocyte lipolysis via activation of the nicotinic acid receptor GPR109A (HM74a/PUMA-G).
18983141 2008 Nicotinic acid receptor agonists.
18787507 2008 Pharmacological effects of lipid-lowering drugs recapitulate with a larger amplitude the phenotypic effects of common variants within their target genes.
18639743 2008 The high-affinity niacin receptor HM74A is decreased in the anterior cingulate cortex of individuals with schizophrenia.
17932499 2008 Neutrophil apoptosis mediated by nicotinic acid receptors (GPR109A).
16674924 2006 Enhancement of arachidonic acid signaling pathway by nicotinic acid receptor HM74A.
16018973 2005 Niacin mediates lipolysis in adipose tissue through its G-protein coupled receptor HM74A.
15489334 2004 The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).
12646212 2003 Molecular identification of nicotinic acid receptor.
12522134 2003 Molecular identification of high and low affinity receptors for nicotinic acid.
12477932 2002 Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.
12044878 2002 Identification of G protein-coupled receptor genes from the human genome sequence.
2834384 1988 Presence of three distinct molecular species of Gi protein alpha subunit. Structure of rat cDNAs and human genomic DNAs.