TGR5-Mediated Bile Acid Sensing Controls Glucose Homeostasis

Charles Thomas, Antimo Gioiello, Lilia G. Noriega, +10

Cell Metabolism

BiochemistryBiliary TractLiver PhysiologyPhysiologyDiabetes +4

6α-Ethyl-Chenodeoxycholic Acid (6-ECDCA), a Potent and Selective FXR Agonist Endowed with Anticholestatic Activity

Roberto Pellicciari, Stefano Fiorucci, Emidio Camaioni, +6

Journal of Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistrySelective Fxr AgonistPharmaceutical ScienceOxysterol +12

TGR5 Activation Inhibits Atherosclerosis by Reducing Macrophage Inflammation and Lipid Loading

Thijs W.H. Pols, Mitsunori Nomura, Taoufiq Harach, +9

Cell Metabolism

InflammationVascular DiseaseImmunologyEndothelial DysfunctionChronic Inflammation +7

The nuclear receptor SHP mediates inhibition of hepatic stellate cells by FXR and protects against liver fibrosis

Stefano Fiorucci, Elisabetta Antonelli, Giovanni Rizzo, +6

Gastroenterology

FibrosisSignal TransductionHepatologyLiver FibrosisHepatic Stellate Cells +13

Family-wide chemical profiling and structural analysis of PARP and tankyrase inhibitors

E. Wahlberg, T. Karlberg, E. Kouznetsova, +12

Nature Biotechnology

Medicinal ChemistryDrug TargetTankyrase InhibitorsBiochemistryMedicine +11

De novo NAD+ synthesis enhances mitochondrial function and improves health

Elena Katsyuba, Adrienne Mottis, Marika Ziętak, +16

Nature

Mitochondrial FunctionBiochemistryMitochondrial DynamicMitochondrial BiologyMetabolic Remodeling +6

Bile Acids Signal via TGR5 to Activate Intestinal Stem Cells and Epithelial Regeneration

Giovanni Sorrentino, Alessia Perino, Gaby El Alam, +4

Gastroenterology

Structural Basis for Bile Acid Binding and Activation of the Nuclear Receptor FXR

Li-Zhi Mi, Srikripa Devarakonda, Joel M. Harp, +5

Molecular Cell

Bile Acid BindingSignal TransductionBiochemistryG Protein-coupled ReceptorNatural Sciences +10

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

Hiroyuki Sato, Antonio Macchiarulo, Charles Thomas, +7

Journal of Medicinal Chemistry

Discovery of 6α-Ethyl-23(<i>S</i>)-methylcholic Acid (<i>S</i>-EMCA, INT-777) as a Potent and Selective Agonist for the TGR5 Receptor, a Novel Target for Diabesity

Roberto Pellicciari, Antimo Gioiello, Antonio Macchiarulo, +9

Journal of Medicinal Chemistry

Pharmaceutical SciencePharmaceutical ChemistryMolecular PharmacologyMedicinal ChemistryOxysterol +16