Patented TGR5 modulators: a review (2006 – present)

Bile acid receptors as targets for the treatment of dyslipidemia and cardiovascular disease

(2012) Geoffrey Porez et al.   JOURNAL OF LIPID RESEARCH

Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators

(2012) Roberto Pellicciari et al.   ACS Medicinal Chemistry Letters

Effects of Chemical Modification of Ursodeoxycholic Acid on TGR5 Activation

(2011) Yusuke Iguchi et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

TGR5 Activation Inhibits Atherosclerosis by Reducing Macrophage Inflammation and Lipid Loading

(2011) Thijs W.H. Pols et al.   Cell Metabolism

NF-κB, Inflammation, and Metabolic Disease

(2011) Rebecca G. Baker et al.   Cell Metabolism

The G-Protein-coupled bile acid receptor, Gpbar1 (TGR5), negatively regulates hepatic inflammatory response through antagonizing nuclear factor kappa light-chain enhancer of activated B cells (NF-κB) in mice

(2011) Yan-Dong Wang et al.   HEPATOLOGY

Dual farnesoid X receptor/TGR5 agonist INT-767 reduces liver injury in the Mdr2 −/− (Abcb4 −/− ) mouse cholangiopathy model by promoting biliary HCO 3− output

(2011) Anna Baghdasaryan et al.   HEPATOLOGY

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

(2011) Tingting Li et al.   MOLECULAR ENDOCRINOLOGY

GLP-1 analogues and insulin: sound the wedding bells?

(2011) Michael A. Nauck et al.   Nature Reviews Endocrinology

Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5

(2010) Mark R. Herbert et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and structure–activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists

(2010) Brian W. Budzik et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Redefining the TGR5 Triterpenoid Binding Pocket at the C-3 Position

(2010) Cédric Genet et al.   ChemMedChem

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

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

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

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

Functional Characterization of the Semisynthetic Bile Acid Derivative INT-767, a Dual Farnesoid X Receptor and TGR5 Agonist

(2010) G. Rizzo et al.   MOLECULAR PHARMACOLOGY

Missing link identified: GpBAR1 is a neuronal bile acid receptor

(2010) S. J. Keely   NEUROGASTROENTEROLOGY AND MOTILITY

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

Weight and Type 2 Diabetes after Bariatric Surgery: Systematic Review and Meta-analysis

(2009) Henry Buchwald et al.   AMERICAN JOURNAL OF MEDICINE

TGR5-Mediated Bile Acid Sensing Controls Glucose Homeostasis

(2009) Charles Thomas et al.   Cell Metabolism

Incretin-Based Therapy of Type 2 Diabetes Mellitus

(2009) Filip Knop et al.   CURRENT PROTEIN & PEPTIDE SCIENCE

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

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

Serum bile acid along with plasma incretins and serum high–molecular weight adiponectin levels are increased after bariatric surgery

(2009) Hiroshi Nakatani et al.   METABOLISM-CLINICAL AND EXPERIMENTAL

Obesity, inflammation, and atherosclerosis

(2009) Viviane Z. Rocha et al.   Nature Reviews Cardiology

Surgical Treatment of Obesity — Weighing the Facts

(2009) Malcolm K. Robinson   NEW ENGLAND JOURNAL OF MEDICINE

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

Oleanolic acid is a selective farnesoid X receptor modulator

(2009) Wenming Liu et al.   PHYTOTHERAPY RESEARCH

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

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

Targeting bile-acid signalling for metabolic diseases

(2008) Charles Thomas et al.   NATURE REVIEWS DRUG DISCOVERY