The Bile Acid Membrane Receptor TGR5: A Valuable Metabolic Target

Macrophages, Inflammation, and Insulin Resistance

(2010) Jerrold M. Olefsky et al.   Annual Review of Physiology

The membrane-bound bile acid receptor TGR5 (Gpbar-1) is localized in the primary cilium of cholangiocytes

(2010) Verena Keitel et al.   BIOLOGICAL CHEMISTRY

Metabolic Networks of Longevity

(2010) Riekelt H. Houtkooper et al.   CELL

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

(2010) Verena Keitel et al.   GLIA

Hypertrophic cardiomyopathy and dysregulation of cardiac energetics in a mouse model of biliary fibrosis

(2010) Moreshwar S. Desai et al.   HEPATOLOGY

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

(2010) Galya Vassileva et al.   JOURNAL OF ENDOCRINOLOGY

Hydrophobic bile salts inhibit gallbladder smooth muscle function via stimulation of GPBAR1 receptors and activation of KATPchannels

(2010) Brigitte Lavoie et al.   JOURNAL OF PHYSIOLOGY-LONDON

Expression and function of the bile acid receptor GpBAR1 (TGR5) in the murine enteric nervous system

(2010) D. P. Poole et al.   NEUROGASTROENTEROLOGY AND MOTILITY

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

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

(2009) George Perides et al.   GASTROENTEROLOGY

The membrane-bound bile acid receptor TGR5 is localized in the epithelium of human gallbladders

(2009) Verena Keitel et al.   HEPATOLOGY

Kupffer cells in non-alcoholic fatty liver disease: The emerging view

(2009) György Baffy   JOURNAL OF HEPATOLOGY

Discovery of 3-Aryl-4-isoxazolecarboxamides as TGR5 Receptor Agonists

(2009) Karen A. Evans et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Structure−Activity Relationship Study of Betulinic Acid, A Novel and Selective TGR5 Agonist, and Its Synthetic Derivatives: Potential Impact in Diabetes¶

(2009) Cédric Genet et al.   JOURNAL OF MEDICINAL CHEMISTRY

Preliminary report: genetic variation within the GPBAR1 gene is not associated with metabolic traits in white subjects at an increased risk for type 2 diabetes mellitus

(2009) Karsten Müssig et al.   METABOLISM-CLINICAL AND EXPERIMENTAL

Serum Bile Acids Are Higher in Humans With Prior Gastric Bypass: Potential Contribution to Improved Glucose and Lipid Metabolism

(2009) Mary-Elizabeth Patti et al.   Obesity

Expression and function of the bile acid receptor TGR5 in Kupffer cells

(2008) Verena Keitel et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Molecular Field Analysis and 3D-Quantitative Structure−Activity Relationship Study (MFA 3D-QSAR) Unveil Novel Features of Bile Acid Recognition at TGR5

(2008) Antonio Macchiarulo et al.   Journal of Chemical Information and Modeling

Fifty years of advances in bile acid synthesis and metabolism

(2008) David W. Russell   JOURNAL OF LIPID RESEARCH

Novel Potent and Selective Bile Acid Derivatives as TGR5 Agonists: Biological Screening, Structure−Activity Relationships, and Molecular Modeling Studies

(2008) Hiroyuki Sato et al.   JOURNAL OF MEDICINAL CHEMISTRY

Metabolic profiling of the human response to a glucose challenge reveals distinct axes of insulin sensitivity

(2008) Oded Shaham et al.   Molecular Systems Biology

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