Therapeutic potential of Takeda-G-protein-receptor-5 (TGR5) agonists. Hope or hype?

Sa1918 TGR5, a Bile Acid Receptor, Is Highly Expressed in Esophageal Adenocarcinoma and Precancerous Lesions Significantly Associated With Worse Overall Survival and Gender Difference

(2015) Chunhong Pang et al.   GASTROENTEROLOGY

The role of bile acids in reducing the metabolic complications of obesity after bariatric surgery: a systematic review

(2015) N C Penney et al.   INTERNATIONAL JOURNAL OF OBESITY

Aberrant DNA Methylation of G-protein-coupled Bile Acid Receptor Gpbar1 (TGR5) is a Potential Biomarker for Hepatitis B Virus Associated Hepatocellular Carcinoma

(2014) Li-Yan Han et al.   International Journal of Medical Sciences

Novel Gut-Based Pharmacology of Metformin in Patients with Type 2 Diabetes Mellitus

(2014) Antonella Napolitano et al.   PLoS One

Microbiota Modification with Probiotics Induces Hepatic Bile Acid Synthesis via Downregulation of the Fxr-Fgf15 Axis in Mice

(2014) Chiara Degirolamo et al.   Cell Reports

Bacterial Metabolite Indole Modulates Incretin Secretion from Intestinal Enteroendocrine L Cells

(2014) Catalin Chimerel et al.   Cell Reports

Release of GLP-1 and PYY in response to the activation of G protein-coupled bile acid receptor TGR5 is mediated by Epac/PLC-ε pathway and modulated by endogenous H2S

(2014) Vanitha Bala et al.   Frontiers in Physiology

The TGR5 receptor mediates bile acid–induced itch and analgesia

(2013) Farzad Alemi et al.   JOURNAL OF CLINICAL INVESTIGATION

The bile acid membrane receptor TGR5: a novel pharmacological target in metabolic, inflammatory and neoplastic disorders

(2013) Vanesa Stepanov et al.   JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION

Bile acid receptors as targets for drug development

(2013) Frank G. Schaap et al.   Nature Reviews Gastroenterology & Hepatology

Sex Differences in the Gut Microbiome Drive Hormone-Dependent Regulation of Autoimmunity

(2013) J. G. M. Markle et al.   SCIENCE

Activation of transmembrane bile acid receptor TGR5 stimulates insulin secretion in pancreatic β cells

(2012) Divya P. Kumar et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Bile acids: From digestion to cancers

(2012) Marine Baptissart et al.   BIOCHIMIE

Chenodeoxycholic acid through a TGR5-dependent CREB signaling activation enhances Cyclin D1 expression and promotes human endometrial cancer cell proliferation

(2012) Ivan Casaburi et al.   CELL CYCLE

Patented TGR5 modulators: a review (2006 – present)

(2012) Antimo Gioiello et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

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

Gender-Divergent Profile of Bile Acid Homeostasis during Aging of Mice

(2012) Zidong Donna Fu et al.   PLoS One

The potential for selective pharmacological therapies through biased receptor signaling

(2012) Terry Kenakin   BMC Pharmacology & Toxicology

The G Protein-Coupled Bile Acid Receptor, TGR5, Stimulates Gallbladder Filling

(2011) Tingting Li et al.   MOLECULAR ENDOCRINOLOGY

Overall Mortality, Incremental Life Expectancy, and Cause of Death at 25 Years in the Program on the Surgical Control of the Hyperlipidemias

(2010) Henry Buchwald et al.   ANNALS OF SURGERY

Bile Acids as Regulators of Hepatic Lipid and Glucose Metabolism

(2010) Michael Trauner et al.   DIGESTIVE DISEASES

The bile acid receptor TGR5 (Gpbar-1) acts as a neurosteroid receptor in brain

(2010) Verena Keitel et al.   GLIA

Gender-dependent effect of Gpbar1 genetic deletion on the metabolic profiles of diet-induced obese mice

(2010) Galya Vassileva et al.   JOURNAL OF ENDOCRINOLOGY

The bile acid membrane receptor TGR5 as an emerging target in metabolism and inflammation

(2010) Thijs W.H. Pols et al.   JOURNAL OF HEPATOLOGY

TGR5-Mediated Bile Acid Sensing Controls Glucose Homeostasis

(2009) Charles Thomas et al.   Cell Metabolism

Biliary Acute Pancreatitis in Mice is Mediated by the G-Protein−Coupled Cell Surface Bile Acid Receptor Gpbar1

(2009) George Perides et al.   GASTROENTEROLOGY

Role of a novel bile acid receptor TGR5 in the development of oesophageal adenocarcinoma

(2009) J. Hong et al.   GUT