Bile acid receptors as targets for drug development
The intracellular nuclear receptor farnesoid X receptor and the transmembrane G protein-
coupled receptor TGR5 respond to bile acids by activating transcriptional networks and/or …
coupled receptor TGR5 respond to bile acids by activating transcriptional networks and/or …
Bile acid receptors as targets for the treatment of dyslipidemia and cardiovascular disease: Thematic review series: New lipid and lipoprotein targets for the treatment …
G Porez, J Prawitt, B Gross, B Staels - Journal of lipid research, 2012 - ASBMB
Dyslipidemia is an important risk factor for cardiovascular disease (CVD) and
atherosclerosis. When dyslipidemia coincides with other metabolic disorders such as …
atherosclerosis. When dyslipidemia coincides with other metabolic disorders such as …
Discovery of tropifexor (LJN452), a highly potent non-bile acid FXR agonist for the treatment of cholestatic liver diseases and nonalcoholic steatohepatitis (NASH)
DC Tully, PV Rucker, D Chianelli, J Williams, A Vidal… - 2017 - ACS Publications
The farnesoid X receptor (FXR) is a nuclear receptor that acts as a master regulator of bile
acid metabolism and signaling. Activation of FXR inhibits bile acid synthesis and increases …
acid metabolism and signaling. Activation of FXR inhibits bile acid synthesis and increases …
Farnesoid X receptor targeting to treat nonalcoholic steatohepatitis
L Adorini, M Pruzanski, D Shapiro - Drug discovery today, 2012 - Elsevier
Nonalcoholic fatty liver disease (NAFLD) is a highly prevalent chronic liver condition
evolving in a proportion of patients into nonalcoholic steatohepatitis (NASH), an aggressive …
evolving in a proportion of patients into nonalcoholic steatohepatitis (NASH), an aggressive …
Intestinal farnesoid X receptor controls transintestinal cholesterol excretion in mice
JF de Boer, M Schonewille, M Boesjes, H Wolters… - Gastroenterology, 2017 - Elsevier
Background & Aims The role of the intestine in the maintenance of cholesterol homeostasis
increasingly is recognized. Fecal excretion of cholesterol is the last step in the …
increasingly is recognized. Fecal excretion of cholesterol is the last step in the …
[HTML][HTML] Rhizoma Coptidis alkaloids alleviate hyperlipidemia in B6 mice by modulating gut microbiota and bile acid pathways
K He, Y Hu, H Ma, Z Zou, Y Xiao, Y Yang… - … et Biophysica Acta (BBA …, 2016 - Elsevier
It is hypothesized that Rhizoma Coptidis (RC) alkaloids exert their hypolipidemic effects
primarily by targeting the gastrointestinal tract and liver. Thus, this study was conducted to …
primarily by targeting the gastrointestinal tract and liver. Thus, this study was conducted to …
FXR modulators for enterohepatic and metabolic diseases
ABSTRACT Introduction: Farnesoid X receptor (FXR), a nuclear receptor mainly expressed
in enterohepatic tissues, is a master for bile acid, lipid and glucose homeostasis …
in enterohepatic tissues, is a master for bile acid, lipid and glucose homeostasis …
FXR: structures, biology, and drug development for NASH and fibrosis diseases
S Tian, S Chen, C Pan, Y Li - Acta Pharmacologica Sinica, 2022 - nature.com
The nuclear receptor farnesoid-X-receptor (FXR) plays an essential role in bile acid,
glucose, and lipid homeostasis. In the last two decades, several diseases, such as obesity …
glucose, and lipid homeostasis. In the last two decades, several diseases, such as obesity …
Modulation of bile acid metabolism to improve plasma lipid and lipoprotein profiles
B Zhang, F Kuipers, JF de Boer… - Journal of clinical …, 2021 - mdpi.com
New drugs targeting bile acid metabolism are currently being evaluated in clinical studies for
their potential to treat cholestatic liver diseases, non-alcoholic fatty liver disease (NAFLD) …
their potential to treat cholestatic liver diseases, non-alcoholic fatty liver disease (NAFLD) …
FXR controls the tumor suppressor NDRG2 and FXR agonists reduce liver tumor growth and metastasis in an orthotopic mouse xenograft model
U Deuschle, J Schüler, A Schulz, T Schlüter, O Kinzel… - 2012 - journals.plos.org
The farnesoid X receptor (FXR) is expressed predominantly in tissues exposed to high
levels of bile acids and controls bile acid and lipid homeostasis. FXR−/− mice develop …
levels of bile acids and controls bile acid and lipid homeostasis. FXR−/− mice develop …