G Protein–Coupled Receptors Targeting Insulin Resistance, Obesity, and Type 2 Diabetes Mellitus

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Type 2 diabetes as an inflammatory disease

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Monocyte recruitment during infection and inflammation

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Association analyses of 249,796 individuals reveal 18 new loci associated with body mass index

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Cardiovascular effects of intensive lifestyle intervention in type 2 diabetes

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Endoplasmic reticulum stress and the inflammatory basis of metabolic disease

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Macrophages, inflammation, and insulin resistance

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Cellular mechanisms of insulin resistance

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The NLRP3 inflammasome instigates obesity-induced inflammation and insulin resistance

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Endocrine regulation of energy metabolism by the skeleton

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

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The Orphan G Protein-coupled Receptors GPR41 and GPR43 Are Activated by Propionate and Other Short Chain Carboxylic Acids

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Adverse metabolic and cardiovascular consequences of circadian misalignment

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Mechanisms for Insulin Resistance: Common Threads and Missing Links

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Inflammation as a link between obesity, metabolic syndrome and type 2 diabetes

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Microvascular and Macrovascular Complications of Diabetes

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Unexpected evidence for active brown adipose tissue in adult humans

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Islet cell failure in type 2 diabetes

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

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

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Insulin and insulin resistance:

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The gut microbiota suppresses insulin-mediated fat accumulation via the short-chain fatty acid receptor GPR43

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Liraglutide once a day versus exenatide twice a day for type 2 diabetes: a 26-week randomised, parallel-group, multinational, open-label trial (LEAD-6)

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CCR2 modulates inflammatory and metabolic effects of high-fat feeding

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CCR2 modulates inflammatory and metabolic effects of high-fat feeding

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Regulation of immune cell function by short‐chain fatty acids

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Macrophage-mediated inflammation in metabolic disease

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GLP-1 receptor agonists for individualized treatment of type 2 diabetes mellitus

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Macrophage Immunometabolism: Where Are We (Going)?

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Critical roles for CCR2 and MCP-3 in monocyte mobilization from bone marrow and recruitment to inflammatory sites

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The NLRP3 Inflammasome: A Sensor for Metabolic Danger?

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Impaired monocyte migration and reduced type 1 (Th1) cytokine responses in C-C chemokine receptor 2 knockout mice.

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Molecular Characterization of the Human β 3 -Adrenergic Receptor

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NAFLD, NASH and liver cancer

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Beta Cell Dysfunction and Insulin Resistance

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The arcuate nucleus mediates GLP-1 receptor agonist liraglutide-dependent weight loss

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Plasma Insulin Responses to Oral and Intravenous Glucose: Studies in Normal and Diabetic Subjects*

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Diet, metabolites, and “western-lifestyle” inflammatory diseases

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Molecular mechanisms of insulin resistance in humans and their potential links with mitochondrial dysfunction

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Virtual and biomolecular screening converge on a selective agonist for GPR30

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Variants in MTNR1B influence fasting glucose levels

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

Lyssenko, V., Nagorny, C. L. F., Erdos, M. R., Wierup, N., Jonsson, A., Spégel, P., Bugliani, M., Saxena, R., Fex, M., Pulizzi, N., et al. (2009) · Nature Genetics · doi:10.1038/ng.288 · Cited by 742 · see citing works

Adherence to Therapies in Patients with Type 2 Diabetes

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Atypical β-adrenoceptor on brown adipocytes as target for anti-obesity drugs

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Cellular and molecular players in adipose tissue inflammation in the development of obesity-induced insulin resistance

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Anatomical Profiling of G Protein-Coupled Receptor Expression

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Effects of once‐weekly semaglutide on appetite, energy intake, control of eating, food preference and body weight in subjects with obesity

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Targeting inflammation in the treatment of type 2 diabetes: time to start

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Targeting adipose tissue in the treatment of obesity-associated diabetes

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A new glucagon and GLP-1 co-agonist eliminates obesity in rodents

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Endocrine Regulation of Male Fertility by the Skeleton

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

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Pharmacological Inhibition of the Chemokine CCL2 (MCP-1) Diminishes Liver Macrophage Infiltration and Steatohepatitis in Chronic Hepatic Injury

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From NAFLD to NASH to cirrhosis—new insights into disease mechanisms

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GPCR-Mediated Signaling of Metabolites

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Cryo-EM structure of the activated GLP-1 receptor in complex with a G protein

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GPR41/FFAR3 and GPR43/FFAR2 as Cosensors for Short-Chain Fatty Acids in Enteroendocrine Cells vs FFAR3 in Enteric Neurons and FFAR2 in Enteric Leukocytes

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In vivo effects of a GPR30 antagonist

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Triggering the succinate receptor GPR91 on dendritic cells enhances immunity

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GPR91 senses extracellular succinate released from inflammatory macrophages and exacerbates rheumatoid arthritis

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The Browning of White Adipose Tissue: Some Burning Issues

Nedergaard, J., & Cannon, B. (2014) · Cell Metabolism · doi:10.1016/j.cmet.2014.07.005 · Cited by 500 · see citing works

Extracellular Ca2+ is a danger signal activating the NLRP3 inflammasome through G protein-coupled calcium sensing receptors

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Once-weekly dulaglutide versus once-daily liraglutide in metformin-treated patients with type 2 diabetes (AWARD-6): a randomised, open-label, phase 3, non-inferiority trial

Dungan, K. M., Povedano, S. T., Forst, T., González, J. G. G., Atisso, C., Sealls, W., & Fahrbach, J. L. (2014) · The Lancet · doi:10.1016/s0140-6736(14)60976-4 · Cited by 486 · see citing works

The Cytokine GM-CSF Drives the Inflammatory Signature of CCR2+ Monocytes and Licenses Autoimmunity

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Pharmacology and functions of receptors for vasoactive intestinal peptide and pituitary adenylate cyclase‐activating polypeptide: IUPHAR Review 1

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Current views on type 2 diabetes

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Update on melatonin receptors: IUPHAR Review 20

Jockers, R., Delagrange, P., Dubocovich, M. L., Markus, R. P., Renault, N., Tosini, G., Cecon, E., & Zlotos, D. P. (2016) · British Journal of Pharmacology · doi:10.1111/bph.13536 · Cited by 426 · see citing works

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

Åhrén, B. (2009) · Nature Reviews Drug Discovery · doi:10.1038/nrd2782 · Cited by 421 · see citing works

Deletion of the G Protein-Coupled Receptor 30 Impairs Glucose Tolerance, Reduces Bone Growth, Increases Blood Pressure, and Eliminates Estradiol-Stimulated Insulin Release in Female Mice

Mårtensson, U. E. A., Salehi, A. A., Windahl, S. H., Gomez, M. F., Swärd, K., Daszkiewicz-Nilsson, J., Wendt, A., Andersson, N., Hellstrand, P., Grände, P., et al. (2008) · Endocrinology · doi:10.1210/en.2008-0623 · Cited by 413 · see citing works

Characterization of the UDP-glucose receptor (re-named here the P2Y14 receptor) adds diversity to the P2Y receptor family

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Glucagon-Like Peptide-1 and Its Class B G Protein–Coupled Receptors: A Long March to Therapeutic Successes

Graaf, C. D., Donnelly, D., Wootten, D., Lau, J., Sexton, P. M., Miller, L. J., Ahn, J.-M., Liao, J., Fletcher, M. M., Yang, D., et al. (2016) · Pharmacological Reviews · doi:10.1124/pr.115.011395 · Cited by 403 · see citing works

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

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GPR119 Is Essential for Oleoylethanolamide-Induced Glucagon-Like Peptide-1 Secretion From the Intestinal Enteroendocrine L-Cell

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Targeting fatty acid and carbohydrate oxidation — A novel therapeutic intervention in the ischemic and failing heart

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Neuronal GLP1R mediates liraglutide’s anorectic but not glucose-lowering effect

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A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice

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Medium-chain Fatty Acids as Ligands for Orphan G Protein-coupled Receptor GPR84*

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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

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G Protein-Coupled Receptor 43 Is Essential for Neutrophil Recruitment during Intestinal Inflammation

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Melatonin secretion and the incidence of type 2 diabetes

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BLT1 and BLT2: the leukotriene B4 receptors

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Rare MTNR1B variants impairing melatonin receptor 1B function contribute to type 2 diabetes

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