Islet G protein-coupled receptors as potential targets for treatment of type 2 diabetes (Q37443837)

20 August 2017

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title

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

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G protein-coupled receptor

20 August 2017

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1

Bo Ahrén

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20 August 2017

14 April 2009

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Nature Reviews Drug Discovery

20 August 2017

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20 August 2017

8

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20 August 2017

369-385

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20 August 2017

5

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https://scigraph.springernature.com/pub.10.1038/nrd2782

20 August 2017

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31 March 2020

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Antidiabetogenic effect of glucagon-like peptide-1 (7-36)amide in normal subjects and patients with diabetes mellitus

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31 March 2020

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Effects of exenatide (exendin-4) on glycemic control and weight over 30 weeks in metformin-treated patients with type 2 diabetes

31 March 2020

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Effects of exenatide (exendin-4) on glycemic control over 30 weeks in patients with type 2 diabetes treated with metformin and a sulfonylurea

31 March 2020

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Exenatide effects on diabetes, obesity, cardiovascular risk factors and hepatic biomarkers in patients with type 2 diabetes treated for at least 3 years

31 March 2020

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Targeting Incretins in Type 2 Diabetes: Role of GLP-1 Receptor Agonists and DPP-4 Inhibitors

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Liraglutide versus glimepiride monotherapy for type 2 diabetes (LEAD-3 Mono): a randomised, 52-week, phase III, double-blind, parallel-treatment trial

31 March 2020

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Efficacy and safety comparison of liraglutide, glimepiride, and placebo, all in combination with metformin, in type 2 diabetes: the LEAD (liraglutide effect and action in diabetes)-2 study

31 March 2020

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Pharmacodynamics, pharmacokinetics, safety, and tolerability of albiglutide, a long-acting glucagon-like peptide-1 mimetic, in patients with type 2 diabetes

31 March 2020

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The islet enhancer vildagliptin: mechanisms of improved glucose metabolism

31 March 2020

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Dipeptidyl peptidase 4 inhibition with sitagliptin: a new therapy for type 2 diabetes

31 March 2020

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Effect of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy on glycemic control in patients with type 2 diabetes.

31 March 2020

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Comparison of vildagliptin and rosiglitazone monotherapy in patients with type 2 diabetes: a 24-week, double-blind, randomized trial.

31 March 2020

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Comparison between vildagliptin and metformin to sustain reductions in HbA(1c) over 1 year in drug-naïve patients with Type 2 diabetes

31 March 2020

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Twelve- and 52-week efficacy of the dipeptidyl peptidase IV inhibitor LAF237 in metformin-treated patients with type 2 diabetes

31 March 2020

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Effect of initial combination therapy with sitagliptin, a dipeptidyl peptidase-4 inhibitor, and metformin on glycemic control in patients with type 2 diabetes.

31 March 2020

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Vildagliptin in combination with pioglitazone improves glycaemic control in patients with type 2 diabetes failing thiazolidinedione monotherapy: a randomized, placebo-controlled study.

31 March 2020

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Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin added to ongoing pioglitazone therapy in patients with type 2 diabetes: a 24-week, multicenter, randomized, double-blind, placebo-controlled, parallel-group study.

31 March 2020

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Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, compared with the sulfonylurea, glipizide, in patients with type 2 diabetes inadequately controlled on metformin alone: a randomized, double-blind, non-inferiority trial.

31 March 2020

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Effects of vildagliptin on glucose control in patients with type 2 diabetes inadequately controlled with a sulphonylurea

31 March 2020

1 reference

Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, in patients with type 2 diabetes mellitus inadequately controlled on glimepiride alone or on glimepiride and metformin.

31 March 2020

1 reference

Glucose-lowering activity of the dipeptidyl peptidase-4 inhibitor saxagliptin in drug-naive patients with type 2 diabetes

31 March 2020

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Cloning, functional expression, and chromosomal localization of the human pancreatic islet glucose-dependent insulinotropic polypeptide receptor

31 March 2020

1 reference

Gastric inhibitory polypeptide (GIP) dose-dependently stimulates glucagon secretion in healthy human subjects at euglycaemia

31 March 2020

1 reference

Defective amplification of the late phase insulin response to glucose by GIP in obese Type II diabetic patients

31 March 2020

1 reference

The pathogenesis of NIDDM involves a defective expression of the GIP receptor

31 March 2020

1 reference

Reversal of islet GIP receptor down-regulation and resistance to GIP by reducing hyperglycemia in the Zucker rat

31 March 2020

1 reference

Four weeks of near-normalisation of blood glucose improves the insulin response to glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide in patients with type 2 diabetes

31 March 2020

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Malonyl-CoA signaling, lipid partitioning, and glucolipotoxicity: role in beta-cell adaptation and failure in the etiology of diabetes

31 March 2020

1 reference

Stimulatory short-term effects of free fatty acids on glucagon secretion at low to normal glucose concentrations

31 March 2020

1 reference

The role of long-chain fatty acyl-CoA esters in beta-cell signal transduction

31 March 2020

1 reference

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

31 March 2020

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

31 March 2020

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

31 March 2020

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G protein-coupled receptors and insulin secretion: 119 and counting

31 March 2020

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The free fatty acid receptor GPR40 generates excitement in pancreatic beta-cells

31 March 2020

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GPR119, a novel G protein-coupled receptor target for the treatment of type 2 diabetes and obesity

31 March 2020

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Free fatty acid receptor 1 (FFA(1)R/GPR40) and its involvement in fatty-acid-stimulated insulin secretion.

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

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The long-chain fatty acid receptor, GPR40, and glucolipotoxicity: investigations using GPR40-knockout mice

31 March 2020

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Regulation of the gene encoding GPR40, a fatty acid receptor expressed selectively in pancreatic beta cells

31 March 2020

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GPR40 is expressed in glucagon producing cells and affects glucagon secretion.

31 March 2020

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Reduction in voltage-gated K+ currents in primary cultured rat pancreatic beta-cells by linoleic acids

31 March 2020

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

31 March 2020

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

31 March 2020

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Loss-of-function mutation of the GPR40 gene associates with abnormal stimulated insulin secretion by acting on intracellular calcium mobilization

31 March 2020

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Activation of ATP-sensitive potassium channels in rat pancreatic beta-cells by linoleic acid through both intracellular metabolites and membrane receptor signalling pathway.

31 March 2020

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

31 March 2020

1 reference

The role of G protein-coupled receptor 40 in lipoapoptosis in mouse beta-cell line NIT-1.

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

Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists

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

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

Seven evolutionarily conserved human rhodopsin G protein-coupled receptors lacking close relatives

31 March 2020

1 reference

Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents

31 March 2020

1 reference

N-acylphosphatidylethanolamine-hydrolyzing phospholipase D: a novel enzyme of the beta-lactamase fold family releasing anandamide and other N-acylethanolamines

31 March 2020

1 reference

Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor

31 March 2020

1 reference

Expression and distribution of Gpr119 in the pancreatic islets of mice and rats: predominant localization in pancreatic polypeptide-secreting PP-cells

31 March 2020

1 reference

A role for intestinal endocrine cell-expressed g protein-coupled receptor 119 in glycemic control by enhancing glucagon-like Peptide-1 and glucose-dependent insulinotropic Peptide release

31 March 2020

1 reference

GPR119: "double-dipping" for better glycemic control

31 March 2020

1 reference

Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119

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

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

31 March 2020

1 reference

A gene expression network model of type 2 diabetes links cell cycle regulation in islets with diabetes susceptibility

31 March 2020

1 reference

Cloning and characterization of the rat free fatty acid receptor GPR120: in vivo effect of the natural ligand on GLP-1 secretion and proliferation of pancreatic beta cells.

31 March 2020

1 reference

Autonomic regulation of islet hormone secretion--implications for health and disease

31 March 2020

1 reference

Glucagon receptors on human islet cells contribute to glucose competence of insulin release

31 March 2020

1 reference

Lower blood glucose, hyperglucagonemia, and pancreatic alpha cell hyperplasia in glucagon receptor knockout mice

31 March 2020

1 reference

Glucagon receptor knockout mice display increased insulin sensitivity and impaired beta-cell function

31 March 2020

1 reference

Glucose intolerance is predicted by low insulin secretion and high glucagon secretion: outcome of a prospective study in postmenopausal Caucasian women

31 March 2020

1 reference

Beta- and alpha-cell dysfunction in subjects developing impaired glucose tolerance: outcome of a 12-year prospective study in postmenopausal Caucasian women

31 March 2020

1 reference

Glucagon as a target for the treatment of Type 2 diabetes

31 March 2020

1 reference

New hepatic targets for glycaemic control in diabetes

31 March 2020

1 reference

Immunoneutralization of endogenous glucagon with monoclonal glucagon antibody normalizes hyperglycaemia in moderately streptozotocin-diabetic rats

31 March 2020

1 reference

Human glucagon receptor antagonists based on alkylidene hydrazides

31 March 2020

1 reference

Glucagon receptor antagonism improves islet function in mice with insulin resistance induced by a high-fat diet

31 March 2020

1 reference

The neuropeptide pituitary adenylate cyclase-activating polypeptide and islet function

31 March 2020

1 reference

Role of pituitary adenylate cyclase-activating polypeptide in the pancreatic endocrine system

31 March 2020

1 reference

PAC1 receptor-deficient mice display impaired insulinotropic response to glucose and reduced glucose tolerance.

31 March 2020

1 reference

Vasoactive intestinal polypeptide/pituitary adenylate cyclase-activating peptide receptor 2 deficiency in mice results in growth retardation and increased basal metabolic rate

31 March 2020

1 reference

Engineering novel VPAC2-selective agonists with improved stability and glucose-lowering activity in vivo.

31 March 2020

1 reference

The NPY/AgRP neuron and energy homeostasis

31 March 2020

1 reference

Neuropeptides and their receptors: innovative science providing novel therapeutic targets

31 March 2020

1 reference

Neuropeptide Y receptors; antisecretory control of intestinal epithelial function

31 March 2020

1 reference

Inhibition of glucose stimulated insulin secretion by neuropeptide Y is mediated via the Y1 receptor and inhibition of adenylyl cyclase in RIN 5AH rat insulinoma cells

31 March 2020

1 reference

Different mechanisms are involved in neuropeptide Y-induced pancreatic vasoconstriction and inhibition of insulin secretion

31 March 2020

1 reference

Neuropeptide Y promotes beta-cell replication via extracellular signal-regulated kinase activation

31 March 2020

1 reference

Normal control of growth hormone secretion

31 March 2020

1 reference

Ghrelin: discovery of the natural endogenous ligand for the growth hormone secretagogue receptor

31 March 2020

1 reference

Ghrelin is a growth-hormone-releasing acylated peptide from stomach

31 March 2020

1 reference

Morphological analysis of ghrelin and its receptor distribution in the rat pancreas

31 March 2020

1 reference

Ghrelin is a physiological regulator of insulin release in pancreatic islets and glucose homeostasis

31 March 2020

1 reference

Stomach is a major source of circulating ghrelin, and feeding state determines plasma ghrelin-like immunoreactivity levels in humans.

31 March 2020

1 reference

Expression of ghrelin and of the GH secretagogue receptor by pancreatic islet cells and related endocrine tumors

31 March 2020

1 reference

Ghrelin is present in pancreatic alpha-cells of humans and rats and stimulates insulin secretion

31 March 2020

1 reference

The ghrelin cell: a novel developmentally regulated islet cell in the human pancreas.

31 March 2020

1 reference

Ghrelin gene expression is markedly higher in fetal pancreas compared with fetal stomach: effect of maternal fasting.

31 March 2020

1 reference

Dose-dependent inhibition by ghrelin of insulin secretion in the mouse

31 March 2020

1 reference

Blockade of pancreatic islet-derived ghrelin enhances insulin secretion to prevent high-fat diet-induced glucose intolerance

31 March 2020

1 reference

Ablation of ghrelin improves the diabetic but not obese phenotype of ob/ob mice

31 March 2020

1 reference

Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss.

31 March 2020

1 reference

The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54

31 March 2020

1 reference

A role for kisspeptin in islet function

31 March 2020

1 reference

Kisspeptin-13 inhibits insulin secretion without affecting glucagon or somatostatin release: study in the perfused rat pancreas

31 March 2020

1 reference

Neuropeptidergic versus cholinergic and adrenergic regulation of islet hormone secretion

31 March 2020

1 reference

Inhibition of insulin secretion via distinct signaling pathways in alpha2-adrenoceptor knockout mice

31 March 2020

1 reference

Effects of acute alpha 2-blockade on insulin action and secretion in humans.

31 March 2020

1 reference

Alpha-adrenergic blockade improves glucose-potentiated insulin secretion in non-insulin-dependent diabetes mellitus

31 March 2020

1 reference

Influence of melatonin and serotonin on glucose-stimulated insulin release from perifused rat pancreatic islets in vitro

31 March 2020

1 reference

Identification and functional characterization of melatonin Mel 1a receptors in pancreatic beta cells: potential role in incretin-mediated cell function by sensitization of cAMP signaling

31 March 2020

1 reference

Melatonin inhibits insulin secretion and decreases PKA levels without interfering with glucose metabolism in rat pancreatic islets.

31 March 2020

1 reference

Evidence for the expression of both the MT1- and in addition, the MT2-melatonin receptor, in the rat pancreas, islet and beta-cell

31 March 2020

1 reference

Melatonin and type 2 diabetes - a possible link?

31 March 2020

1 reference

Common variant in MTNR1B associated with increased risk of type 2 diabetes and impaired early insulin secretion

31 March 2020

1 reference

Variants in MTNR1B influence fasting glucose levels

31 March 2020

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A variant near MTNR1B is associated with increased fasting plasma glucose levels and type 2 diabetes risk

31 March 2020

1 reference

A critical role for beta cell M3 muscarinic acetylcholine receptors in regulating insulin release and blood glucose homeostasis in vivo

31 March 2020

1 reference

Role of the M3 muscarinic acetylcholine receptor in beta-cell function and glucose homeostasis

31 March 2020

1 reference

Muscarinic acetylcholine receptors: mutant mice provide new insights for drug development

31 March 2020

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The endocannabinoid system in obesity and type 2 diabetes.

31 March 2020

1 reference

The endocannabinoid system and rimonabant: a new drug with a novel mechanism of action involving cannabinoid CB1 receptor antagonism--or inverse agonism--as potential obesity treatment and other therapeutic use.

31 March 2020

1 reference

Cannabinoid receptors regulate Ca(2+) signals and insulin secretion in pancreatic beta-cell.

31 March 2020

1 reference

Endocannabinoid dysregulation in the pancreas and adipose tissue of mice fed with a high-fat diet

31 March 2020

1 reference

Cannabinoids inhibit insulin secretion and cytosolic Ca2+ oscillation in islet beta-cells via CB1 receptors

31 March 2020

1 reference

Presence of functional cannabinoid receptors in human endocrine pancreas

31 March 2020

1 reference

Activation of cannabinoid CB1 receptors induces glucose intolerance in rats.

31 March 2020

1 reference

Efficacy and tolerability of rimonabant in overweight or obese patients with type 2 diabetes: a randomised controlled study

31 March 2020

1 reference

Efficacy and safety of the weight-loss drug rimonabant: a meta-analysis of randomised trials

31 March 2020

1 reference

Purinergic receptors on insulin-secreting cells

31 March 2020

1 reference

P2Y receptor activation enhances insulin release from pancreatic beta-cells by triggering the cyclic AMP/protein kinase A pathway

31 March 2020

1 reference

Expression of purinergic P2Y receptor subtypes by INS-1 insulinoma beta-cells: a molecular and binding characterization.

31 March 2020

1 reference

Uridine diphosphate (UDP) stimulates insulin secretion by activation of P2Y6 receptors

31 March 2020

1 reference

Purinergic and pyrimidinergic receptors as potential drug targets

31 March 2020

1 reference

Purinergic receptors in the endocrine and exocrine pancreas.

31 March 2020

1 reference

2-thioether 5'-O-(1-thiotriphosphate)adenosine derivatives as new insulin secretagogues acting through P2Y-Receptors

31 March 2020

1 reference

Cloning and characterization of two human G protein-coupled receptor genes (GPR38 and GPR39) related to the growth hormone secretagogue and neurotensin receptors

31 March 2020

1 reference

Obestatin, a peptide encoded by the ghrelin gene, opposes ghrelin's effects on food intake

31 March 2020

1 reference

Is GPR39 the natural receptor of obestatin?

31 March 2020

1 reference

GPR39 signaling is stimulated by zinc ions but not by obestatin

31 March 2020

1 reference

Incretin-based therapies in type 2 diabetes mellitus

31 March 2020

1 reference

Novel combination treatment of type 2 diabetes DPP-4 inhibition + metformin

31 March 2020

1 reference

Sulfonylurea Compounds Uncouple the Glucose Dependence of the Insulinotropic Effect of Glucagon-Like Peptide 1

31 March 2020

1 reference

Calcium and apoptosis: ER-mitochondria Ca2+ transfer in the control of apoptosis

31 March 2020

1 reference

Analysis of gene expression in pancreatic islets from diet-induced obese mice

31 March 2020

1 reference

Potentiated beta-cell response to non-glucose stimuli in insulin-resistant C57BL/6J mice.

31 March 2020

1 reference

Iterative stimulation of pancreatic islets by glipizide

31 March 2020

1 reference

Dose-response for glycaemic and metabolic changes 28 days after single injection of long-acting release exenatide in diabetic fatty Zucker rats

31 March 2020

1 reference

Allosteric modulation of heterodimeric G-protein-coupled receptors.

31 March 2020

1 reference

High throughput screening for orphan and liganded GPCRs

31 March 2020

1 reference

The G protein-coupled receptor subset of the rat genome

31 March 2020

1 reference

GPCR deorphanizations: the novel, the known and the unexpected transmitters

31 March 2020

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International Union of Pharmacology. XLVI. G protein-coupled receptor list.

31 March 2020

1 reference

G-protein coupled receptor structure

31 March 2020

1 reference

31 March 2020

1 reference

The Physiology of Glucagon-like Peptide 1

31 March 2020

1 reference

Dorothy Hodgkin Lecture 2008. Gastric inhibitory polypeptide (GIP) revisited: a new therapeutic target for obesity-diabetes?

31 March 2020

1 reference

Fatty acid binding receptors and their physiological role in type 2 diabetes

31 March 2020

1 reference

Free fatty acid receptors and drug discovery

31 March 2020

1 reference

A family of fatty acid binding receptors

31 March 2020

1 reference

Class II G protein-coupled receptors for VIP and PACAP: structure, models of activation and pharmacology.

31 March 2020

1 reference

Kisspeptins: a multifunctional peptide system with a role in reproduction, cancer and the cardiovascular system

31 March 2020

1 reference

Progress in developing cholecystokinin (CCK)/gastrin receptor ligands that have therapeutic potential

31 March 2020

1 reference

Molecular mechanisms of beta2-adrenergic receptor function and regulation

31 March 2020

1 reference

Agonists and antagonists targeting the different alpha2-adrenoceptor subtypes

31 March 2020

1 reference

Melatonin receptors, heterodimerization, signal transduction and binding sites: what's new?

31 March 2020

1 reference

Metabolic roles of the M3 muscarinic acetylcholine receptor studied with M3 receptor mutant mice: a review

31 March 2020

1 reference

Molecular, pharmacological and clinical aspects of liraglutide, a once-daily human GLP-1 analogue

31 March 2020

1 reference

Regulatory roles for small G proteins in the pancreatic beta-cell: lessons from models of impaired insulin secretion

31 March 2020

1 reference

12 December 2020

Distribution of glucagon receptors on hormone-specific endocrine cells of rat pancreatic islets

1 reference

12 December 2020

Effectiveness and side effects of thiazolidinediones for type 2 diabetes: real-life experience from a tertiary hospital.

1 reference

12 December 2020

Evidence for a circadian rhythm of insulin secretion

1 reference

12 December 2020

Altered gastrointestinal and metabolic function in the GPR39-obestatin receptor-knockout mouse

1 reference

12 December 2020

Cholecystokinin and the regulation of insulin secretion

1 reference

12 December 2020

G-protein-coupled receptors: molecular mechanisms involved in receptor activation and selectivity of G-protein recognition

1 reference

12 December 2020

Intraperitoneal PACAP administration decreases blood glucose in GK rats, and in normal and high fat diet mice

1 reference

12 December 2020

Impairment of the insulinotropic effect of gastric inhibitory polypeptide (GIP) in obese and diabetic rats is related to the down-regulation of its pancreatic receptors

1 reference

12 December 2020

Probing cell type-specific functions of Gi in vivo identifies GPCR regulators of insulin secretion.

1 reference

12 December 2020

Efficacy and tolerability of vildagliptin vs. pioglitazone when added to metformin: a 24-week, randomized, double-blind study

1 reference

12 December 2020

Antidiabetogenic action of cholecystokinin-8 in type 2 diabetes

1 reference

12 December 2020

Cell and molecular biology of the incretin hormones glucagon-like peptide-I and glucose-dependent insulin releasing polypeptide.

1 reference

12 December 2020

GCRDb: a G-protein-coupled receptor database

1 reference

12 December 2020

Glucose-dependent insulinotropic polypeptide is a growth factor for beta (INS-1) cells by pleiotropic signaling

1 reference

12 December 2020

Effects of exenatide (exendin-4) on glycemic control over 30 weeks in sulfonylurea-treated patients with type 2 diabetes

1 reference

12 December 2020

A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release

1 reference

12 December 2020

Alogliptin, a potent and selective dipeptidyl peptidase-IV inhibitor for the treatment of type 2 diabetes

1 reference

12 December 2020

Pituitary adenylate cyclase-activating polypeptide stimulates insulin and glucagon secretion in humans

1 reference

12 December 2020

Melatonin, endocrine pancreas and diabetes.

1 reference

12 December 2020

Increased insulin secretion and normalization of glucose tolerance by cholinergic agonism in high fat-fed mice.

1 reference

12 December 2020

Identifiers

DOI

10.1038/NRD2782

1 reference

20 August 2017

1 reference

PubMed ID

19365392