G protein-coupled receptors for energy metabolites as new therapeutic targets (Q38025858)

27 August 2017

G protein-coupled receptors for energy metabolites as new therapeutic targets (English)

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G protein-coupled receptor

27 August 2017

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Stefan Offermanns

3

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author name string

Clara C Blad

series ordinal

1

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PubMed ID

22790105

27 August 2017

Cong Tang

series ordinal

2

1 reference

27 August 2017

13 July 2012

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Nature Reviews Drug Discovery

27 August 2017

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27 August 2017

11

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27 August 2017

603-619

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27 August 2017

8

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https://scigraph.springernature.com/pub.10.1038/nrd3777

27 August 2017

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Seven transmembrane receptors: something old, something new.

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How do receptors activate G proteins?

31 March 2020

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Mammalian G proteins and their cell type specific functions

31 March 2020

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The skinny on fat: lipolysis and fatty acid utilization in adipocytes

31 March 2020

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Regulation of adipose tissue lipolysis revisited

31 March 2020

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Islet G protein-coupled receptors as potential targets for treatment of type 2 diabetes

31 March 2020

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A gut feeling for obesity: 7TM sensors on enteroendocrine cells

31 March 2020

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G-protein-coupled receptors in intestinal chemosensation

31 March 2020

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Obesity, inflammation, and atherosclerosis

31 March 2020

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Inflammatory links between obesity and metabolic disease

31 March 2020

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Macrophages, inflammation, and insulin resistance

31 March 2020

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The cellular and signaling networks linking the immune system and metabolism in disease

31 March 2020

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The receptors for mammalian sweet and umami taste

31 March 2020

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Allosteric modulation of family C G-protein-coupled receptors: from molecular insights to therapeutic perspectives

31 March 2020

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Mammalian sweet taste receptors

31 March 2020

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Human receptors for sweet and umami taste

31 March 2020

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The sweet taste of true synergy: positive allosteric modulation of the human sweet taste receptor

31 March 2020

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Distinct contributions of T1R2 and T1R3 taste receptor subunits to the detection of sweet stimuli

31 March 2020

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Different functional roles of T1R subunits in the heteromeric taste receptors

31 March 2020

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Identification of the cyclamate interaction site within the transmembrane domain of the human sweet taste receptor subunit T1R3.

31 March 2020

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Molecular mechanism of species-dependent sweet taste toward artificial sweeteners

31 March 2020

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Molecular mechanism for the umami taste synergism

31 March 2020

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Gut-expressed gustducin and taste receptors regulate secretion of glucagon-like peptide-1

31 March 2020

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T1r3 and alpha-gustducin in gut regulate secretion of glucagon-like peptide-1.

31 March 2020

1 reference

The role of the gut sweet taste receptor in regulating GLP-1, PYY, and CCK release in humans

31 March 2020

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T1R3 and gustducin in gut sense sugars to regulate expression of Na+-glucose cotransporter 1

31 March 2020

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Glucose sensing in L cells: a primary cell study

31 March 2020

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Taste-signaling proteins are coexpressed in solitary intestinal epithelial cells.

31 March 2020

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Molecular mechanisms underlying nutrient-stimulated incretin secretion

31 March 2020

1 reference

Sweet taste receptor signaling in beta cells mediates fructose-induced potentiation of glucose-stimulated insulin secretion.

31 March 2020

1 reference

Positive allosteric modulators of the human sweet taste receptor enhance sweet taste

31 March 2020

1 reference

Molecular mechanism of the sweet taste enhancers

31 March 2020

1 reference

Lactisole interacts with the transmembrane domains of human T1R3 to inhibit sweet taste.

31 March 2020

1 reference

The physiology of cellular liporegulation

31 March 2020

1 reference

Free fatty acid receptors FFAR1 and GPR120 as novel therapeutic targets for metabolic disorders.

31 March 2020

1 reference

The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids

31 March 2020

1 reference

Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40.

31 March 2020

1 reference

A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs

31 March 2020

1 reference

Gpr40 is expressed in enteroendocrine cells and mediates free fatty acid stimulation of incretin secretion

31 March 2020

1 reference

Production and characterization of a monoclonal antibody against GPR40 (FFAR1; free fatty acid receptor 1)

31 March 2020

1 reference

Taste Preference for Fatty Acids Is Mediated by GPR40 and GPR120

31 March 2020

1 reference

Expression of free fatty acid receptor GPR40 in the central nervous system of adult monkeys.

31 March 2020

1 reference

Expression of the gene for a membrane-bound fatty acid receptor in the pancreas and islet cell tumours in humans: evidence for GPR40 expression in pancreatic beta cells and implications for insulin secretion

31 March 2020

1 reference

The FFA receptor GPR40 links hyperinsulinemia, hepatic steatosis, and impaired glucose homeostasis in mouse

31 March 2020

1 reference

The fatty acid receptor GPR40 plays a role in insulin secretion in vivo after high-fat feeding.

31 March 2020

1 reference

Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice

31 March 2020

1 reference

GPR40 is necessary but not sufficient for fatty acid stimulation of insulin secretion in vivo.

31 March 2020

1 reference

Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules

31 March 2020

1 reference

Synthesis and biological evaluation of 3-aryl-3-(4-phenoxy)-propionic acid as a novel series of G protein-coupled receptor 40 agonists

31 March 2020

1 reference

Overexpression of GPR40 in pancreatic beta-cells augments glucose-stimulated insulin secretion and improves glucose tolerance in normal and diabetic mice

31 March 2020

1 reference

Glucose activates free fatty acid receptor 1 gene transcription via phosphatidylinositol-3-kinase-dependent O-GlcNAcylation of pancreas-duodenum homeobox-1

31 March 2020

1 reference

Synthesis and activity of small molecule GPR40 agonists.

31 March 2020

1 reference

Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469.

31 March 2020

1 reference

Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties.

31 March 2020

1 reference

3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists

31 March 2020

1 reference

AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents

31 March 2020

1 reference

AMG 837: a potent, orally bioavailable GPR40 agonist.

31 March 2020

1 reference

TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats

31 March 2020

1 reference

Design, synthesis, and biological activity of potent and orally available G protein-coupled receptor 40 agonists

31 March 2020

1 reference

Identification of fused-ring alkanoic acids with improved pharmacokinetic profiles that act as G protein-coupled receptor 40/free fatty acid receptor 1 agonists.

31 March 2020

1 reference

Optimization of (2,3-dihydro-1-benzofuran-3-yl)acetic acids: discovery of a non-free fatty acid-like, highly bioavailable G protein-coupled receptor 40/free fatty acid receptor 1 agonist as a glucose-dependent insulinotropic agent.

31 March 2020

1 reference

Discovery of phenylpropanoic acid derivatives containing polar functionalities as potent and orally bioavailable G protein-coupled receptor 40 agonists for the treatment of type 2 diabetes.

31 March 2020

1 reference

TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial

31 March 2020

1 reference

Uncovering the pharmacology of the G protein-coupled receptor GPR40: high apparent constitutive activity in guanosine 5'-O-(3-[35S]thio)triphosphate binding studies reflects binding of an endogenous agonist

31 March 2020

1 reference

The action and mode of binding of thiazolidinedione ligands at free fatty acid receptor 1

31 March 2020

1 reference

Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists

31 March 2020

1 reference

A novel class of antagonists for the FFAs receptor GPR40.

31 March 2020

1 reference

Discovery of novel agonists and antagonists of the free fatty acid receptor 1 (FFAR1) using virtual screening

31 March 2020

1 reference

Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists

31 March 2020

1 reference

Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120

31 March 2020

1 reference

Cloning, expression, and pharmacological characterization of the GPR120 free fatty acid receptor from cynomolgus monkey: comparison with human GPR120 splice variants

31 March 2020

1 reference

G protein-coupled receptors in human fat taste perception

31 March 2020

1 reference

Differential signaling by splice variants of the human free fatty acid receptor GPR120.

31 March 2020

1 reference

The regulation of adipogenesis through GPR120.

31 March 2020

1 reference

GPR120 is an omega-3 fatty acid receptor mediating potent anti-inflammatory and insulin-sensitizing effects

31 March 2020

1 reference

Distribution and regulation of protein expression of the free fatty acid receptor GPR120.

31 March 2020

1 reference

Targeting GPR120 and other fatty acid-sensing GPCRs ameliorates insulin resistance and inflammatory diseases

31 March 2020

1 reference

Dysfunction of lipid sensor GPR120 leads to obesity in both mouse and human

31 March 2020

1 reference

Structure-activity relationships of GPR120 agonists based on a docking simulation.

31 March 2020

1 reference

Discovery of a potent and selective GPR120 agonist.

31 March 2020

1 reference

Medium-chain fatty acids as ligands for orphan G protein-coupled receptor GPR84

31 March 2020

1 reference

G protein-coupled receptor 84, a microglia-associated protein expressed in neuroinflammatory conditions

31 March 2020

1 reference

The G-protein coupled receptor, GPR84 regulates IL-4 production by T lymphocytes in response to CD3 crosslinking

31 March 2020

1 reference

Inflammatory changes in adipose tissue enhance expression of GPR84, a medium-chain fatty acid receptor: TNFα enhances GPR84 expression in adipocytes

31 March 2020

1 reference

Short-chain fatty acids and human colonic function: roles of resistant starch and nonstarch polysaccharides

31 March 2020

1 reference

The Orphan G protein-coupled receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids

31 March 2020

1 reference

Functional characterization of human receptors for short chain fatty acids and their role in polymorphonuclear cell activation

31 March 2020

1 reference

Identification of a free fatty acid receptor, FFA2R, expressed on leukocytes and activated by short-chain fatty acids

31 March 2020

1 reference

Acetate and propionate short chain fatty acids stimulate adipogenesis via GPCR43

31 March 2020

1 reference

Short-chain fatty acids stimulate leptin production in adipocytes through the G protein-coupled receptor GPR41

31 March 2020

1 reference

Roles of GPR41 and GPR43 in leptin secretory responses of murine adipocytes to short chain fatty acids

31 March 2020

1 reference

Short-chain fatty acids and ketones directly regulate sympathetic nervous system via G protein-coupled receptor 41 (GPR41)

31 March 2020

1 reference

Improved glucose control and reduced body fat mass in free fatty acid receptor 2-deficient mice fed a high-fat diet

31 March 2020

1 reference

Short-chain fatty acid receptor, GPR43, is expressed by enteroendocrine cells and mucosal mast cells in rat intestine

31 March 2020

1 reference

Expression of short-chain fatty acid receptor GPR41 in the human colon.

31 March 2020

1 reference

Effects of the gut microbiota on host adiposity are modulated by the short-chain fatty-acid binding G protein-coupled receptor, Gpr41

31 March 2020

1 reference

Expression of the short-chain fatty acid receptor, GPR43, in the human colon.

31 March 2020

1 reference

Density distribution of free fatty acid receptor 2 (FFA2)-expressing and GLP-1-producing enteroendocrine L cells in human and rat lower intestine, and increased cell numbers after ingestion of fructo-oligosaccharide

31 March 2020

1 reference

Short-chain fatty acids stimulate glucagon-like peptide-1 secretion via the G-protein-coupled receptor FFAR2

31 March 2020

1 reference

Butyrate and propionate protect against diet-induced obesity and regulate gut hormones via free fatty acid receptor 3-independent mechanisms

31 March 2020

1 reference

Regulation of inflammatory responses by gut microbiota and chemoattractant receptor GPR43

31 March 2020

1 reference

LSSIG is a novel murine leukocyte-specific GPCR that is induced by the activation of STAT3

31 March 2020

1 reference

SCFAs induce mouse neutrophil chemotaxis through the GPR43 receptor

31 March 2020

1 reference

G protein-coupled receptor 43 is essential for neutrophil recruitment during intestinal inflammation

31 March 2020

1 reference

Activation of G protein-coupled receptor 43 in adipocytes leads to inhibition of lipolysis and suppression of plasma free fatty acids

31 March 2020

1 reference

The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators

31 March 2020

1 reference

Identification and functional characterization of allosteric agonists for the G protein-coupled receptor FFA2.

31 March 2020

1 reference

Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3

31 March 2020

1 reference

Role of GPR81 in lactate-mediated reduction of adipose lipolysis

31 March 2020

1 reference

Lactate inhibits lipolysis in fat cells through activation of an orphan G-protein-coupled receptor, GPR81

31 March 2020

1 reference

(D)-beta-Hydroxybutyrate inhibits adipocyte lipolysis via the nicotinic acid receptor PUMA-G.

31 March 2020

1 reference

Deorphanization of GPR109B as a receptor for the beta-oxidation intermediate 3-OH-octanoic acid and its role in the regulation of lipolysis

31 March 2020

1 reference

International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B).

31 March 2020

1 reference

An autocrine lactate loop mediates insulin-dependent inhibition of lipolysis through GPR81.

31 March 2020

1 reference

PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect

31 March 2020

1 reference

Neutrophil apoptosis mediated by nicotinic acid receptors (GPR109A)

31 March 2020

1 reference

Enhancement of arachidonic acid signaling pathway by nicotinic acid receptor HM74A

31 March 2020

1 reference

Elucidation of signaling and functional activities of an orphan GPCR, GPR81.

31 March 2020

1 reference

Aromatic D-amino acids act as chemoattractant factors for human leukocytes through a G protein-coupled receptor, GPR109B

31 March 2020

1 reference

Molecular identification of nicotinic acid receptor

31 March 2020

1 reference

Molecular identification of high and low affinity receptors for nicotinic acid

31 March 2020

1 reference

Nicotinic acid receptor agonists differentially activate downstream effectors

31 March 2020

1 reference

Nicotinic acid-induced flushing is mediated by activation of epidermal langerhans cells

31 March 2020

1 reference

Regulation of phosphoinositide phospholipases by hormones, neurotransmitters, and other agonists linked to G proteins

31 March 2020

1 reference

Peroxisome proliferator-activated receptor gamma regulates expression of the anti-lipolytic G-protein-coupled receptor 81 (GPR81/Gpr81).

31 March 2020

1 reference

Inflammation inhibits GPR81 expression in adipose tissue

31 March 2020

1 reference

Lactate release from the subcutaneous tissue in lean and obese men.

31 March 2020

1 reference

Lactate release from adipose tissue and skeletal muscle in vivo: defective insulin regulation in insulin-resistant obese women

31 March 2020

1 reference

3,5-Dihydroxybenzoic acid, a specific agonist for hydroxycarboxylic acid 1, inhibits lipolysis in adipocytes.

31 March 2020

1 reference

GPR109A (PUMA-G/HM74A) mediates nicotinic acid-induced flushing

31 March 2020

1 reference

Langerhans cells release prostaglandin D2 in response to nicotinic acid

31 March 2020

1 reference

PUMA-G, an IFN-gamma-inducible gene in macrophages is a novel member of the seven transmembrane spanning receptor superfamily

31 March 2020

1 reference

Nicotinic acid- and monomethyl fumarate-induced flushing involves GPR109A expressed by keratinocytes and COX-2-dependent prostanoid formation in mice

31 March 2020

1 reference

GPR109A is a G-protein-coupled receptor for the bacterial fermentation product butyrate and functions as a tumor suppressor in colon

31 March 2020

1 reference

Colonic gene expression in conventional and germ-free mice with a focus on the butyrate receptor GPR109A and the butyrate transporter SLC5A8.

31 March 2020

1 reference

GPR109A as an anti-inflammatory receptor in retinal pigment epithelial cells and its relevance to diabetic retinopathy

31 March 2020

1 reference

Liver and kidney metabolism during prolonged starvation

31 March 2020

1 reference

Direct Regulatory Effect of Ketones on Lipolysis and on Glucose Concentrations in Man

31 March 2020

1 reference

Nicotinic acid: pharmacological effects and mechanisms of action

31 March 2020

1 reference

Regression of coronary artery disease as a result of intensive lipid-lowering therapy in men with high levels of apolipoprotein B

31 March 2020

1 reference

Simvastatin and niacin, antioxidant vitamins, or the combination for the prevention of coronary disease

31 March 2020

1 reference

Extended-release niacin or ezetimibe and carotid intima-media thickness.

31 March 2020

1 reference

Fifteen year mortality in Coronary Drug Project patients: long-term benefit with niacin

31 March 2020

1 reference

Reduction of mortality in the Stockholm Ischaemic Heart Disease Secondary Prevention Study by combined treatment with clofibrate and nicotinic acid

31 March 2020

1 reference

Anti-inflammatory effects of nicotinic acid in human monocytes are mediated by GPR109A dependent mechanisms

31 March 2020

1 reference

Effects of colestipol-niacin therapy on human femoral atherosclerosis

31 March 2020

1 reference

Effects of high-dose modified-release nicotinic acid on atherosclerosis and vascular function: a randomized, placebo-controlled, magnetic resonance imaging study

31 March 2020

1 reference

A randomized trial of a strategy for increasing high-density lipoprotein cholesterol levels: effects on progression of coronary heart disease and clinical events

31 March 2020

1 reference

Niacin in patients with low HDL cholesterol levels receiving intensive statin therapy

31 March 2020

1 reference

Is niacin ineffective? Or did AIM-HIGH miss its target?

31 March 2020

1 reference

Fibrate use in diabetes: new concepts

31 March 2020

1 reference

Studies on the Effect of Nicotinic Acid on Catecholamine Stimulated Lipolysis in Adipose Tissue in Vitro

31 March 2020

1 reference

Is raising HDL a futile strategy for atheroprotection?

31 March 2020

1 reference

Critical role of cholesterol ester transfer protein in nicotinic acid-mediated HDL elevation in mice

31 March 2020

1 reference

Niacin increases HDL by reducing hepatic expression and plasma levels of cholesteryl ester transfer protein in APOE*3Leiden.CETP mice.

31 March 2020

1 reference

Antiatherogenic small, dense HDL--guardian angel of the arterial wall?

31 March 2020

1 reference

The nicotinic acid receptor GPR109A (HM74A or PUMA-G) as a new therapeutic target

31 March 2020

1 reference

Modulation of HDL metabolism by the niacin receptor GPR109A in mouse hepatocytes

31 March 2020

1 reference

Mechanism of action of niacin

31 March 2020

1 reference

Effects of a niacin receptor partial agonist, MK-0354, on plasma free fatty acids, lipids, and cutaneous flushing in humans

31 March 2020

1 reference

(1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (MK-1903): a potent GPR109a agonist that lowers free fatty acids in humans

31 March 2020

1 reference

Nicotinic acid (niacin): new lipid-independent mechanisms of action and therapeutic potentials

31 March 2020

1 reference

Nicotinic acid inhibits progression of atherosclerosis in mice through its receptor GPR109A expressed by immune cells

31 March 2020

1 reference

Evidence that niacin inhibits acute vascular inflammation and improves endothelial dysfunction independent of changes in plasma lipids

31 March 2020

1 reference

Niacin stimulates adiponectin secretion through the GPR109A receptor

31 March 2020

1 reference

Extended-release niacin raises adiponectin and leptin

31 March 2020

1 reference

Niacin inhibits skin dendritic cell mobilization in a GPR109A independent manner but has no impact on monocyte trafficking in atherosclerosis

31 March 2020

1 reference

Nicotinic acid has anti-atherogenic and anti-inflammatory properties on advanced atherosclerotic lesions independent of its lipid-modifying capabilities

31 March 2020

1 reference

The mechanism and mitigation of niacin-induced flushing

31 March 2020

1 reference

Antagonism of the prostaglandin D2 receptor 1 suppresses nicotinic acid-induced vasodilation in mice and humans

31 March 2020

1 reference

Effects of laropiprant on nicotinic acid-induced flushing in patients with dyslipidemia

31 March 2020

1 reference

beta-Arrestin1 mediates nicotinic acid-induced flushing, but not its antilipolytic effect, in mice

31 March 2020

1 reference

Teaching old receptors new tricks: biasing seven-transmembrane receptors

31 March 2020

1 reference

The psoriasis drug monomethylfumarate is a potent nicotinic acid receptor agonist

31 March 2020

1 reference

Dimethyl fumarate for multiple sclerosis.

31 March 2020

1 reference

Trial watch: Phase III success for Biogen's oral multiple sclerosis therapy

31 March 2020

1 reference

Niaspan treatment improves neurological functional recovery in experimental autoimmune encephalomyelitis mice

31 March 2020

1 reference

Fumaric acid esters are effective in chronic experimental autoimmune encephalomyelitis and suppress macrophage infiltration

31 March 2020

1 reference

Inhibition of lipolysis by nicotinic acid and by acipimox

31 March 2020

1 reference

Evaluation of the lipid-lowering activity of AY-25,712 in rats

31 March 2020

1 reference

Nicotinic acid receptor subtypes and their ligands

31 March 2020

1 reference

Pyrazole derivatives as partial agonists for the nicotinic acid receptor

31 March 2020

1 reference

Agonist lead identification for the high affinity niacin receptor GPR109a

31 March 2020

1 reference

Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a

31 March 2020

1 reference

3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice.

31 March 2020

1 reference

Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).

31 March 2020

1 reference

GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109a

31 March 2020

1 reference

Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemia.

31 March 2020

1 reference

GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a

31 March 2020

1 reference

Phenolic acids suppress adipocyte lipolysis via activation of the nicotinic acid receptor GPR109A (HM74a/PUMA-G).

31 March 2020

1 reference

Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A).

31 March 2020

1 reference

Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.

31 March 2020

1 reference

Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.

31 March 2020

1 reference

Anthranilic acid replacements in a niacin receptor agonist

31 March 2020

1 reference

Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonists

31 March 2020

1 reference

Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.

31 March 2020

1 reference

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

31 March 2020

1 reference

Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: optimization of in vitro activity

31 March 2020

1 reference

Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A.

31 March 2020

1 reference

Novel 3,6,7-substituted pyrazolopyrimidines as positive allosteric modulators for the hydroxycarboxylic acid receptor 2 (GPR109A).

31 March 2020

1 reference

Nicotinic acid receptor agonists

31 March 2020

1 reference

HM74a agonists: will they be the new generation of nicotinic acid?

31 March 2020

1 reference

Acyl hydroxypyrazoles as novel agonists for high-affinity nicotinic acid receptor GPR109A: WO2008051403.

31 March 2020

1 reference

Novel patent publications on high-affinity nicotinic acid receptor agonists

31 March 2020

1 reference

Molecular cloning of cDNAs encoding a LD78 receptor and putative leukocyte chemotactic peptide receptors

31 March 2020

1 reference

cDNA representational difference analysis of human neutrophils stimulated by GM-CSF

31 March 2020

1 reference

GPR109A, GPR109B and GPR81, a family of hydroxy-carboxylic acid receptors

31 March 2020

1 reference

Evidence for constitutive dimerization of niacin receptor subtypes

31 March 2020

1 reference

Triglyceride modulation by acifran analogs: activity towards the niacin high and low affinity G protein-coupled receptors HM74A and HM74.

31 March 2020

1 reference

Analogues of acifran: agonists of the high and low affinity niacin receptors, GPR109a and GPR109b

31 March 2020

1 reference

1-Alkyl-benzotriazole-5-carboxylic acids are highly selective agonists of the human orphan G-protein-coupled receptor GPR109b.

31 March 2020

1 reference

3-Nitro-4-amino benzoic acids and 6-amino nicotinic acids are highly selective agonists of GPR109b.

31 March 2020

1 reference

5-N,N-Disubstituted 5-aminopyrazole-3-carboxylic acids are highly potent agonists of GPR109b.

31 March 2020

1 reference

The succinate receptor as a novel therapeutic target for oxidative and metabolic stress-related conditions

31 March 2020

1 reference

Citric acid cycle intermediates as ligands for orphan G-protein-coupled receptors

31 March 2020

1 reference

The succinate receptor GPR91 in neurons has a major role in retinal angiogenesis

31 March 2020

1 reference

Triggering the succinate receptor GPR91 on dendritic cells enhances immunity

31 March 2020

1 reference

Activation of the succinate receptor GPR91 in macula densa cells causes renin release.

31 March 2020

1 reference

Gene expression profiling for the identification of G-protein coupled receptors in human platelets.

31 March 2020

1 reference

Anatomical profiling of G protein-coupled receptor expression

31 March 2020

1 reference

High glucose and renin release: the role of succinate and GPR91.

31 March 2020

1 reference

Localization of the succinate receptor in the distal nephron and its signaling in polarized MDCK cells

31 March 2020

1 reference

Discovery of a potent and selective small molecule hGPR91 antagonist.

31 March 2020

1 reference

GPR99, a new G protein-coupled receptor with homology to a new subgroup of nucleotide receptors

31 March 2020

1 reference

GPR80/99, proposed to be the P2Y(15) receptor activated by adenosine and AMP, is not a P2Y receptor.

31 March 2020

1 reference

Simultaneous quantitative determination of alpha-ketoglutaric acid and 5-hydroxymethylfurfural in human plasma by gas chromatography-mass spectrometry

31 March 2020

1 reference

31 March 2020

Lipolysis in adipocytes

1 reference

FAT SIGNALS--lipases and lipolysis in lipid metabolism and signaling

31 March 2020

1 reference

Characterization of determinants of ligand binding to the nicotinic acid receptor GPR109A (HM74A/PUMA-G).

31 March 2020

1 reference

Lactate production in adipose tissue: a regulated function with extra-adipose implications

31 March 2020

1 reference

12 December 2020

Alkylresorcinol metabolites in urine correlate with the intake of whole grains and cereal fibre in free-living Swedish adults.

1 reference

12 December 2020

Roles of short-chain fatty acids receptors, GPR41 and GPR43 on colonic functions.

1 reference

12 December 2020

Succinate receptor GPR91 provides a direct link between high glucose levels and renin release in murine and rabbit kidney

1 reference

12 December 2020

Coding of sweet, bitter, and umami tastes: different receptor cells sharing similar signaling pathways

1 reference

12 December 2020

Expression and localization of GPR109A (PUMA-G/HM74A) mRNA and protein in mammalian retinal pigment epithelium.

1 reference

12 December 2020

Clofibrate and niacin in coronary heart disease

1 reference

12 December 2020

Addition of quantitative 3-hydroxy-octadecanoic acid to the stable isotope gas chromatography-mass spectrometry method for measuring 3-hydroxy fatty acids.

1 reference

12 December 2020

Simultaneous analysis of plasma free fatty acids and their 3-hydroxy analogs in fatty acid beta-oxidation disorders

1 reference

12 December 2020

Beneficial effects of combined colestipol-niacin therapy on coronary atherosclerosis and coronary venous bypass grafts

1 reference

12 December 2020

Nicotinic acid: an old drug with a promising future

1 reference

12 December 2020

Recent progress in the discovery of niacin receptor agonists.

1 reference

12 December 2020

Identifiers

DOI

10.1038/NRD3777

1 reference

27 August 2017

1 reference

PubMed ID

22790105