Novel Small Molecule Agonist of TGR5 Possesses Anti-Diabetic Effects but Causes Gallbladder Filling in Mice
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Title
Novel Small Molecule Agonist of TGR5 Possesses Anti-Diabetic Effects but Causes Gallbladder Filling in Mice
Authors
Keywords
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Journal
PLoS One
Volume 10, Issue 8, Pages e0136873
Publisher
Public Library of Science (PLoS)
Online
2015-08-28
DOI
10.1371/journal.pone.0136873
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Note: Only part of the references are listed.- 4-Benzofuranyloxynicotinamide derivatives are novel potent and orally available TGR5 agonists
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- Discovery of Trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as Potent, Orally Bioavailable TGR5 (GPBAR1) Agonists: Structure–Activity Relationships, Lead Optimization, and Chronic In Vivo Efficacy
- (2014) Dean P. Phillips et al. JOURNAL OF MEDICINAL CHEMISTRY
- TRC210258, a novel TGR5 agonist, reduces glycemic and dyslipidemic cardiovascular risk in animal models of diabesity
- (2013) Shitalkumar Zambad et al. Diabetes Metabolic Syndrome and Obesity-Targets and Therapy
- Design, Synthesis, and Antidiabetic Activity of 4-Phenoxynicotinamide and 4-Phenoxypyrimidine-5-carboxamide Derivatives as Potent and Orally Efficacious TGR5 Agonists
- (2012) Hongliang Duan et al. JOURNAL OF MEDICINAL CHEMISTRY
- The G Protein-Coupled Bile Acid Receptor, TGR5, Stimulates Gallbladder Filling
- (2011) Tingting Li et al. MOLECULAR ENDOCRINOLOGY
- Nutrient detection by incretin hormone secreting cells
- (2011) Eleftheria Diakogiannaki et al. PHYSIOLOGY & BEHAVIOR
- A new life for bile acids
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- Postprandial plasma bile acid responses in normal weight and obese subjects
- (2010) C. Glicksman et al. ANNALS OF CLINICAL BIOCHEMISTRY
- TGR5-Mediated Bile Acid Sensing Controls Glucose Homeostasis
- (2009) Charles Thomas et al. Cell Metabolism
- TGR5: an emerging bile acid G-protein-coupled receptor target for the potential treatment of metabolic disorders
- (2009) Atul Tiwari et al. DRUG DISCOVERY TODAY
- The membrane-bound bile acid receptor TGR5 is localized in the epithelium of human gallbladders
- (2009) Verena Keitel et al. HEPATOLOGY
- Discovery of 6α-Ethyl-23(S)-methylcholic Acid (S-EMCA, INT-777) as a Potent and Selective Agonist for the TGR5 Receptor, a Novel Target for Diabesity
- (2009) Roberto Pellicciari et al. JOURNAL OF MEDICINAL CHEMISTRY
- A Gut Feeling for Obesity: 7TM Sensors on Enteroendocrine Cells
- (2008) Maja S. Engelstoft et al. Cell Metabolism
- Targeting bile-acid signalling for metabolic diseases
- (2008) Charles Thomas et al. NATURE REVIEWS DRUG DISCOVERY
- Bile Acids and the Membrane Bile Acid Receptor TGR5—Connecting Nutrition and Metabolism
- (2008) Charles Thomas et al. THYROID
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