Results 91 to 100 of about 2,458 (158)
Discovery of a new class of GPBAR1 modulators
, 2017 Since the discovery of the G-protein-coupled bile acid receptor GPBAR1 (also known as TGR5), there has been an increased interest to pharmacologically modulate this target involved in lipids and glucose metabolism disorders such as nonalcoholic ...Stefano Fiorucci, Carmen Festa, Maria Valeria D’Auria, Simona De Marino, Vittorio Limongelli, Angela Zampella +5 morecore Steroidal scaffolds as FXR and GPBAR1 ligands: from chemistry to therapeutical application
, 2015 Bile acids (BAs) are experiencing a new life. Next to their ancestral roles in lipid digestion and solubilization, BAs are today recognized signaling molecules involved in many physiological functions.Distrutti, Eleonora, Fiorucci, Stefano, Distrutti, E, ZAMPELLA, ANGELA, SEPE, VALENTINA, Limongelli, V, LIMONGELLI, VITTORIO, Sepe, V, Zampella, A.1. +8 morecore +1 more sourceAgonism for the bile acid receptor GPBAR1 reverses liver and vascular damage in a mouse model of steatohepatitis
, 2019 Nonalcoholic steatohepatitis (NASH) is associated with an increased risk of developing cardiovascular complications and mortality, suggesting that treatment of NASH might benefit from combined approaches that target the liver and the cardiovascular ...Distrutti, Eleonora, Fiorucci, Stefano, Bucci, Mariarosaria, Carino, Adriana, Brancaleone, Vincenzo, Monti, Maria Chiara, Fiorucci, Chiara, Vellecco, Valentina, Marchianò, Silvia, Zampella, Angela, Biagioli, Michele +10 morecore +1 more sourceThe bile acid receptor GPBAR1 modulates CCL2/CCR2 signaling at the liver sinusoidal/macrophage interface and reverses acetaminophen-induced liver toxicity
, 2020 Drug-induced liver injury caused by acetaminophen (acetyl-para-aminophenol [APAP]) is the main cause of acute liver failure and liver transplantation in several Western countries.Biagioli M., Fiorucci C., Zampella A., Fiorucci S., Carino A., Distrutti E., Di Giorgio C., Marchianò S., Baldoni M., Bordoni M., Roselli R. +10 morecore +1 more sourceEffects of BAR502 on scratching behavior in GPBAR1+/+ and-/- mice administered with ANIT.
, 2015 GPBAR1+/+ and-/- mice were treated for 10 days with ANIT or with the combination of ANIT plus BAR502. At the end of the treatments mice were subjected to intradermal injection of DCA.Barbara Renga (134135), Claudio D’Amore (770255), Angela Zampella (186821), Valentina Sepe (186788), Stefano Fiorucci (134151), Sabrina Cipriani (134132), Antonio Angelo De Tursi (770257), Maria Chiara Monti (186804), Michele Simonetti (770256), Adriana Carino (277117) +9 morecore +1 more sourceMouse monocytes express GPBAR1 and its agonism reduces LPS-induced cytokine production.
, 2014 (A) Gpbar1 and 18s mRNA levels were assessed by Taqman in C57BL/6 mouse whole blood and isolated leukocytes (n = 2 for leukocytes, n = 5 for blood). (B–C) GPBAR1 protein levels were assessed on mouse blood cells by flow cytometry using CD115 to stain ...Dimitria E. Stefanopoulos (589175), Andre Broermann (589180), F. James King (589173), Louise K. Modis (108347), Josephine Pelletier (589170), Susan M. Lukas (589172), Eugene R. Hickey (589183), Christian Harcken (589182), Donald J. Souza (589171), Jonathan D. Hill (589174), Nuruddeen D. Lewis (192385), Kelli Ryan (589176), Donna Skow (589178), Sudha Desai (589177), Lori A. Patnaude (589169), Daniel Kuzmich (589181), Stefan G. Kauschke (589179) +16 morecore +1 more sourceEpoxide functionalization on cholane side chains in the identification of G-protein coupled bile acid receptor (GPBAR1) selective agonists
, 2017 The G-protein coupled receptor of bile acids GPBAR1 is a bile acid receptor that plays an important role in regulating innate immunity, glucose homeostasis and energy expenditure representing an interesting target for the treatment of metabolic and ...Fiorucci, Stefano, Adriana Carino, Dario Masullo, Marchianò, Silvia, Simona De Marino, Valentina Sepe, Vittorio Limongelli, MASULLO, DARIO, Angela Zampella, Silvia Marchianò, DE MARINO, SIMONA, Claudia Finamore, Carino, Adriana, Francesco Saverio Di Leva, FINAMORE, CLAUDIA, Stefano Fiorucci, ZAMPELLA, ANGELA, SEPE, VALENTINA, Di Leva, Francesco Saverio, LIMONGELLI, VITTORIO +19 morecore +2 more sourcesG-Protein-coupled Bile Acid Receptor 1 (GPBAR1, TGR5) agonists reduce the production of pro-inflammatory cytokines and stabilize the alternative macrophage phenotype
, 2014 GPBAR1 (also known as TGR5) is a G protein-coupled receptor (GPCR), which triggers intracellular signals upon ligation by various bile acids. The receptor has been studied mainly for its function in energy expenditure and glucose homeostasis, and there ...Bouhelal, Rochdi, Raad, Layla, Arista, Luca, Carballido, Jose, Hoegenauer, Klemens, Werner, Gudrun, Nguyen, Deborah G., Schmiedeberg, Niko, Jaksche, Herbert, Bhat, B. Ganesh, Rauld, Celine +10 morecore +1 more sourceG‑Protein-Coupled Bile
Acid Receptor 1 (GPBAR1,
TGR5) Agonists Reduce the Production of Proinflammatory Cytokines
and Stabilize the Alternative Macrophage Phenotype
, 2016 GPBAR1
(also known as TGR5) is a G-protein-coupled receptor (GPCR)
that triggers intracellular signals upon ligation by various bile
acids. The receptor has been studied mainly for its function in energy
expenditure and glucose homeostasis, and there is ...Celine Rauld (1697938), Niko Schmiedeberg (1697923), José
M. Carballido (1697950), Deborah G. Nguyen (1697944), B. Ganesh Bhat (1697926), Gudrun Werner (1697929), Klemens Högenauer (1697947), Herbert Jaksche (1697932), Layla Raad (1697935), Rochdi Bouhelal (1697941), Luca Arista (1463827) +10 morecore +1 more sourceGpbar1 agonism promotes a Pgc-1α-dependent browning of white adipose tissue and energy expenditure and reverses diet-induced steatohepatitis in mice
, 2017 Gpbar1 is a bile acid activated receptor for secondary bile acids. Here we have investigated the mechanistic role of Gpbar1 in the regulation of adipose tissues functionality in a murine model of steatohepatitis (NASH).Fiorucci, Stefano, MONTI, Maria Chiara, Cipriani, Sabrina, Cipriani, S., Michele Biagioli, Zampella, A., Maria Chiara Monti, Silvia Marchianò, Monti, M. C., Stefano Fiorucci, Zampella, Angela, Fiorucci, S., Adriana Carino, Paolo Scarpelli, Marchianò, Silvia, Scarpelli, Paolo, Biagioli, M., Angela Zampella, Biagioli, Michele, Carino, Adriana, Carino, A., Sabrina Cipriani, Scarpelli, P., Marchianã2, Silvia, Marchian(`o), S. +24 morecore +1 more source
