Results 211 to 220 of about 114,798 (264)

Nonacidic Farnesoid X Receptor Modulators

Journal of Medicinal Chemistry, 2017
As a cellular bile acid sensor, farnesoid X receptor (FXR) participates in regulation of bile acid, lipid and glucose homeostasis, and liver protection. Clinical results have validated FXR as therapeutic target in hepatic and metabolic diseases.
Daniel Flesch, Sun-Yee Cheung, Jurema Schmidt, Matthias Gabler, Pascal Heitel, Jan Kramer, Astrid Kaiser, Markus Hartmann, Mara Lindner, Kerstin Lüddens-Dämgen, Jan Heering, Christina Lamers, Hartmut Lüddens, Mario Wurglics, Ewgenij Proschak, Manfred Schubert-Zsilavecz, Daniel Merk   +16 more
openaire   +3 more sources

Antiatherosclerotic effect of farnesoid X receptor

American Journal of Physiology-Heart and Circulatory Physiology, 2009
The farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily that functions as an endogenous sensor for bile acids and regulates cholesterol and fatty acid metabolism. The effect of FXR activation on aortic plaque formation was assessed by feeding apolipoprotein E-deficient (ApoE−/−) mice with the synthetic FXR ligand INT-747, a ...
MENCARELLI, Andrea, RENGA, Barbara, DISTRUTTI, ELEONORA, FIORUCCI, Stefano   +3 more
openaire   +3 more sources

Modulation of the Gut Microbiota-Farnesoid X Receptor Axis Improves Deoxycholic Acid-induced Intestinal Inflammation in Mice.

Journal of Crohn's & Colitis, 2021
BACKGROUND AND AIMS Inflammatory bowel disease (IBD) is associated with gut dysbiosis and dysregulation of bile acid metabolism. A high luminal content of deoxycholic acid (DCA) with consumption of a Westernized diet is implicated in the pathogenesis of ...
Mengque Xu, Yuqin Shen, M. Cen, Yubin Zhu, Fangli Cheng, L. Tang, Xia Zheng, John J Kim, N. Dai, Weiling Hu   +9 more
semanticscholar   +1 more source

Recent Advances in the Medicinal Chemistry of Farnesoid X Receptor.

Journal of Medicinal Chemistry, 2021
Farnesoid X receptor (FXR) is an important regulator of bile acid, lipid, amino acid, and glucose homeostasis, hepatic inflammation, regeneration, and fibrosis.
Yuanying Fang, Lamees Hegazy, B. Finck, Bahaa Elgendy   +3 more
semanticscholar   +1 more source

A nonbile acid farnesoid X receptor agonist tropifexor potently inhibits cholestatic liver injury and fibrosis by modulating the gut–liver axis

Liver international (Print), 2021
Tropifexor (TXR) is a novel nonbile acid that acts as an agonist of farnesoid X receptor (FXR). TXR is currently in Phase 2 trials for the treatment of non‐alcoholic steatohepatitis (NASH).
Yongtao Xiao, Ying Wang, Yang Liu, Weipeng Wang, Xinbei Tian, Shanshan Chen, Ying Lu, Jun Du, W. Cai   +8 more
semanticscholar   +1 more source

Pharmacologic activation of hepatic farnesoid X receptor prevents parenteral nutrition–associated cholestasis in mice

Hepatology, 2021
Parenteral nutrition (PN)–associated cholestasis (PNAC) complicates the care of patients with intestinal failure. In PNAC, phytosterol containing PN synergizes with intestinal injury and IL‐1β derived from activated hepatic macrophages to suppress ...
K. E. El Kasmi, Swati Ghosh, Aimee L. Anderson, M. Devereaux, N. Balasubramaniyan, A. D’Alessandro, D. Orlicky, F. Suchy, C. Shearn, R. Sokol   +9 more
semanticscholar   +1 more source

Dual Agonist of Farnesoid X Receptor and Takeda G Protein‐Coupled Receptor 5 Inhibits Hepatitis B Virus Infection In Vitro and In Vivo

Hepatology, 2021
Chronic HBV infection is a major health problem worldwide. Currently, the first‐line treatment for HBV is nucleos(t)ide analogs or interferons; however, efficient therapeutic approaches that enable cure are lacking.
Kiyoaki Ito, A. Okumura, J. Takeuchi, Koichi Watashi, Rieko Inoue, Taeko Yamauchi, K. Sakamoto, Y. Yamashita, Y. Iguchi, M. Une, T. Wakita, K. Umezawa, M. Yoneda   +12 more
semanticscholar   +1 more source

Progesterone Metabolites as Farnesoid X Receptor Inhibitors

Digestive Diseases, 2015
Sulfated progesterone metabolites rise 100-fold in the third trimester of human pregnancy and have been shown to be elevated further in the gestational disorder intrahepatic cholestasis of pregnancy (ICP). Typical concentrations of progesterone sulfates range from 1 to 10 µmol/L in an uncomplicated pregnancy and rise to approximately 40 µmol/L in ICP ...
Abu-Hayyeh, Shadi, Williamson, Catherine
openaire   +3 more sources

Suppressed farnesoid X receptor by iron overload in mice and humans potentiates iron‐induced hepatotoxicity

Hepatology, 2021
Iron overload (IO) is a frequent finding in the general population. As the major iron storage site, the liver is subject to iron toxicity. Farnesoid X receptor (FXR) regulates bile acid metabolism and is implicated in various liver diseases.
Hui Xiong, Chunze Zhang, Lifeng Han, Tong Xu, Khawar Saeed, Jing Han, Jing Liu, C. Klaassen, F. Gonzalez, Yuanfu Lu, Youcai Zhang   +10 more
semanticscholar   +1 more source