Results 21 to 30 of about 2,458 (158)

Combinatorial targeting of G‐protein‐coupled bile acid receptor 1 and cysteinyl leukotriene receptor 1 reveals a mechanistic role for bile acids and leukotrienes in drug‐induced liver injury

Hepatology, EarlyView., 2022
CHIN117 is a dual cysteinyl leukotriene receptor 1 (CYSLTR1) antagonist and G‐protein‐coupled bile acid receptor 1 (GPBAR1) agonist. In the liver, GPBAR1 and CYSLTR1 are coexpressed by liver sinusoidal endothelial cells (LSECs), HSCs, circulating monocytes/macrophages, and liver resident macrophages (Kupffer cells).
Michele Biagioli, Silvia Marchianò, Cristina di Giorgio, Rosalinda Roselli, Martina Bordoni, Rachele Bellini, Bianca Fiorillo, Valentina Sepe, Bruno Catalanotti, Chiara Cassiano, Maria Chiara Monti, Eleonora Distrutti, Angela Zampella, Stefano Fiorucci   +13 more
wiley   +1 more source

Bile acid activated receptors: Integrating immune and metabolic regulation in non-alcoholic fatty liver disease

Liver Research, 2021
Bile acids are a family of atypical steroids generated at the interface of liver-intestinal microbiota acting on a ubiquitously expressed family of membrane and nuclear receptors known as bile acid activated receptors.
Michele Biagioli, Stefano Fiorucci
doaj   +1 more source

GPBAR1 promotes proliferation and is related to poor prognosis of high-grade glioma via inducing MAFB expression [PDF]

, 2022
Background. Glioma is the most prevalent brain tumors with extremely poor prognosis, but the prognostic biomarkers of high-grade (grade III and IV) gliomas (HGG) are still insufficient. Materials and methods.
Wu, Tao, Li, Huaqing, Guo, Hui, Liang, Nan, Zhang, Chunpu, Sun, Suohui   +5 more
core   +1 more source

(E)-7-Ethylidene-lithocholic Acid (7-ELCA) Is a Potent Dual Farnesoid X Receptor (FXR) Antagonist and GPBAR1 Agonist Inhibiting FXR-Induced Gene Expression in Hepatocytes and Stimulating Glucagon-like Peptide-1 Secretion From Enteroendocrine Cells

Frontiers in Pharmacology, 2021
Bile acids (BAs) are key signaling steroidal molecules that regulate glucose, lipid, and energy homeostasis via interactions with the farnesoid X receptor (FXR) and G-protein bile acid receptor 1 (GPBAR1).
Alzbeta Stefela, Miroslav Kaspar, Miroslav Kaspar, Martin Drastik, Thales Kronenberger, Thales Kronenberger, Stanislav Micuda, Martin Dracinsky, Blanka Klepetarova, Eva Kudova, Petr Pavek   +10 more
doaj   +1 more source

Improving glucose and lipids metabolism: drug development based on bile acid related targets

Cell Stress, 2021
Bariatric surgery is one of the most effective treatment options for severe obesity and its comorbidities. However, it is a major surgery that poses several side effects and risks which impede its clinical use.
Hanchen Shen, Lili Ding, Mehdi Baig, Jingyan Tian, Yang Wang, Wendong Huang   +5 more
doaj   +1 more source

Bile acid dysmetabolism in inflammatory bowel diseases

Alʹmanah Kliničeskoj Mediciny, 2023
Aim: To summarize the state-of-the-art data on the molecular mechanisms of bile acid (BA) synthesis and absorption, their impaired absorption and receptor-dependent signaling, as well as on the effects of the gut microbiota on BA metabolism in ...
Daria A. Kuznetsova, Sergey V. Lapin, Irina V. Gubonina   +2 more
doaj   +1 more source

Discovery of BAR502, as potent steroidal antagonist of leukemia inhibitory factor receptor for the treatment of pancreatic adenocarcinoma

Frontiers in Oncology, 2023
IntroductionThe leukemia inhibitory factor (LIF), is a cytokine belonging to IL-6 family, whose overexpression correlate with poor prognosis in cancer patients, including pancreatic ductal adenocarcinoma (PDAC). LIF signaling is mediate by its binding to
Cristina Di Giorgio, Rachele Bellini, Antonio Lupia, Antonio Lupia, Carmen Massa, Martina Bordoni, Silvia Marchianò, Rosalinda Rosselli, Valentina Sepe, Pasquale Rapacciuolo, Federica Moraca, Federica Moraca, Elva Morretta, Patrizia Ricci, Ginevra Urbani, Maria Chiara Monti, Michele Biagioli, Eleonora Distrutti, Bruno Catalanotti, Angela Zampella, Stefano Fiorucci   +20 more
doaj   +1 more source

The bile acid activated receptors GPBAR1 and FXR exert antagonistic effects on autophagy

, 2021
Autophagy is a highly conserved catabolic process activated by fasting and caloric restriction. FXR, a receptor for primary bile acids, reverses the activity of cAMP-response element binding protein (CREB) on autophagy-related genes (Atg)s and terminates
Distrutti, Eleonora, Fiorucci, Stefano, Bordoni, Martina, Carino, Adriana, Monti, Maria Chiara, Fiorucci, Chiara, Marchianò, Silvia, Zampella, Angela, Scarpelli, Paolo, Di Giorgio, Cristina, Roselli, Rosalinda, Biagioli, Michele   +11 more
core   +2 more sources

Discovery of a Potent and Orally Active Dual GPBAR1/CysLT1R Modulator for the Treatment of Metabolic Fatty Liver Disease

Frontiers in Pharmacology, 2022
Nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH) are two highly prevalent human diseases caused by excessive fat deposition in the liver.
Stefano Fiorucci, Pasquale Rapacciuolo, Bianca Fiorillo, Rosalinda Roselli, Silvia Marchianò, Cristina Di Giorgio, Martina Bordoni, Rachele Bellini, Chiara Cassiano, Paolo Conflitti, Bruno Catalanotti, Vittorio Limongelli, Vittorio Limongelli, Valentina Sepe, Michele Biagioli, Angela Zampella   +15 more
doaj   +1 more source

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

, 1989
BACKGROUND: Bile acids (BAs) regulate cells by activating nuclear and membrane-bound receptors. G protein coupled bile acid receptor 1 (GpBAR1) is a membrane-bound G-protein-coupled receptor that can mediate the rapid, transcription-independent actions ...
Corvera, C.U., Pelayo, J.C., F. Cattaruzza, Poole, D.P., Godfrey, C., Cattaruzza, F., D. P. Poole, J. G. Kirkland, N. W. Bunnett, J. C. Pelayo, C. Godfrey, C. U. Corvera, Cottrell, G.S., G. S. Cottrell, Kirkland, J.G., Bunnett, N.W.   +15 more
core   +1 more source