INT-767 prevents NASH and promotes visceral fat brown adipogenesis and mitochondrial function

Brown adipose tissue thermogenic adaptation requires Nrf1-mediated proteasomal activity

(2018) Alexander Bartelt et al.   NATURE MEDICINE

Degradation of brown adipocyte purine nucleotides regulates uncoupling protein 1 activity

(2018) Tobias Fromme et al.   Molecular Metabolism

A dual agonist of farnesoid X receptor (FXR) and the G protein–coupled receptor TGR5, INT-767, reverses age-related kidney disease in mice

(2017) Xiaoxin X. Wang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Farnesoid X receptor induces Takeda G-protein receptor 5 cross-talk to regulate bile acid synthesis and hepatic metabolism

(2017) Preeti Pathak et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Nutrient-sensing nuclear receptors PPARα and FXR control liver energy balance

(2017) Geoffrey A. Preidis et al.   JOURNAL OF CLINICAL INVESTIGATION

Targeting hepatic macrophages to treat liver diseases

(2017) Frank Tacke   JOURNAL OF HEPATOLOGY

Anti-fibrotic effects of chronic treatment with the selective FXR agonist obeticholic acid in the bleomycin-induced rat model of pulmonary fibrosis

(2017) Paolo Comeglio et al.   JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY

Cardiopulmonary protective effects of the selective FXR agonist obeticholic acid in the rat model of monocrotaline-induced pulmonary hypertension

(2017) Linda Vignozzi et al.   JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY

Roles of Diacylglycerols and Ceramides in Hepatic Insulin Resistance

(2017) Max C. Petersen et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

BAR502, a dual FXR and GPBAR1 agonist, promotes browning of white adipose tissue and reverses liver steatosis and fibrosis

(2017) Adriana Carino et al.   Scientific Reports

Systematic review of bariatric surgery liver biopsies clarifies the natural history of liver disease in patients with severe obesity

(2016) Pierre Bedossa et al.   GUT

Tadalafil reduces visceral adipose tissue accumulation by promoting preadipocytes differentiation towards a metabolically healthy phenotype: Studies in rabbits

(2016) Elena Maneschi et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

The Bile Acid Chenodeoxycholic Acid Increases Human Brown Adipose Tissue Activity

(2015) Evie P.M. Broeders et al.   Cell Metabolism

Role of microenvironment on neuroblastoma SK-N-AS SDHB-silenced cell metabolism and function

(2015) E. Rapizzi et al.   ENDOCRINE-RELATED CANCER

Hepatic STAMP2 alleviates high fat diet-induced hepatic steatosis and insulin resistance

(2015) Hye Y. Kim et al.   JOURNAL OF HEPATOLOGY

Farnesoid X nuclear receptor ligand obeticholic acid for non-cirrhotic, non-alcoholic steatohepatitis (FLINT): a multicentre, randomised, placebo-controlled trial

(2015) Brent A Neuschwander-Tetri et al.   LANCET

Intestinal FXR agonism promotes adipose tissue browning and reduces obesity and insulin resistance

(2015) Sungsoon Fang et al.   NATURE MEDICINE

Unraveling the roles of PLIN5: linking cell biology to physiology

(2015) Rachael R. Mason et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Stimulation of soluble guanylyl cyclase protects against obesity by recruiting brown adipose tissue

(2015) Linda S. Hoffmann et al.   Nature Communications

Bile acid flux through portal but not peripheral veins inhibits CYP7A1 expression without involvement of ileal FGF19 in rabbits

(2014) Quan Shang et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

Molecular mechanisms of GLUT4 regulation in adipocytes

(2014) R. Govers   DIABETES & METABOLISM

Nonalcoholic steatohepatitis as a novel player in metabolic syndrome-induced erectile dysfunction: An experimental study in the rabbit

(2014) Linda Vignozzi et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Mitochondrial Dynamics in the Regulation of Nutrient Utilization and Energy Expenditure

(2013) Marc Liesa et al.   Cell Metabolism

Increased cGMP promotes healthy expansion and browning of white adipose tissue

(2013) Michaela M. Mitschke et al.   FASEB JOURNAL

Efficacy and Safety of the Farnesoid X Receptor Agonist Obeticholic Acid in Patients With Type 2 Diabetes and Nonalcoholic Fatty Liver Disease

(2013) Sunder Mudaliar et al.   GASTROENTEROLOGY

Bile Acid Receptor Activation Modulates Hepatic Monocyte Activity and Improves Nonalcoholic Fatty Liver Disease

(2013) Rachel H. McMahan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

FXR activation normalizes insulin sensitivity in visceral preadipocytes of a rabbit model of MetS

(2013) Elena Maneschi et al.   JOURNAL OF ENDOCRINOLOGY

Farnesoid X receptor targeting to treat nonalcoholic steatohepatitis

(2012) Luciano Adorini et al.   DRUG DISCOVERY TODAY

Testosterone treatment improves metabolic syndrome-induced adipose tissue derangements

(2012) Elena Maneschi et al.   JOURNAL OF ENDOCRINOLOGY

Testosterone and farnesoid X receptor agonist INT-747 counteract high fat diet-induced bladder alterations in a rabbit model of metabolic syndrome

(2012) Annamaria Morelli et al.   JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY

Mechanisms of fibrosis: therapeutic translation for fibrotic disease

(2012) Thomas A Wynn et al.   NATURE MEDICINE

Activation of peroxisome proliferator-activated receptor-alpha stimulates both differentiation and fatty acid oxidation in adipocytes

(2011) Tsuyoshi Goto et al.   JOURNAL OF LIPID RESEARCH

A Role of the Bile Salt Receptor FXR in Atherosclerosis

(2010) Jurre Hageman et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Farnesoid X Receptor Activation Prevents the Development of Vascular Calcification in ApoE −/− Mice With Chronic Kidney Disease

(2010) Shinobu Miyazaki-Anzai et al.   CIRCULATION RESEARCH

Mitochondrial dysfunction is induced by high levels of glucose and free fatty acids in 3T3-L1 adipocytes

(2010) Chun-Lin Gao et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

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

TGR5-Mediated Bile Acid Sensing Controls Glucose Homeostasis

(2009) Charles Thomas et al.   Cell Metabolism

Characterization of human adult stem-cell populations isolated from visceral and subcutaneous adipose tissue

(2009) Silvana Baglioni et al.   FASEB JOURNAL

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

Coordinated Regulation of Dimethylarginine Dimethylaminohydrolase-1 and Cationic Amino Acid Transporter-1 by Farnesoid X Receptor in Mouse Liver and Kidney and Its Implication in the Control of Blood Levels of Asymmetric Dimethylarginine

(2009) J. Li et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Testosterone Partially Ameliorates Metabolic Profile and Erectile Responsiveness to PDE5 Inhibitors in an Animal Model of Male Metabolic Syndrome

(2009) Sandra Filippi et al.   Journal of Sexual Medicine

Role of Bile Acids and Bile Acid Receptors in Metabolic Regulation

(2009) Philippe Lefebvre et al.   PHYSIOLOGICAL REVIEWS

Protein Kinase G Controls Brown Fat Cell Differentiation and Mitochondrial Biogenesis

(2009) B. Haas et al.   Science Signaling

Targeting bile-acid signalling for metabolic diseases

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