Ligand activation of the aryl hydrocarbon (AHR) has profound effects upon the immunological status of the gastrointestinal tract, establishing and maintaining signaling networks, which facilitate host-microbe homeostasis at the mucosal interface. However, the identity of the ligand(s) responsible for such AHR-mediated activation within the gut remains to be firmly established....
Polycyclic aromatic hydrocarbons (PAHs) are ubiquitous environmental contaminants generated as byproducts of natural and anthropogenic combustion processes. Despite significant public health concern, physiologically based pharmacokinetic (PBPK) modeling efforts for PAHs have so far been limited to naphthalene, plus simpler PK models for pyrene, nitropyrene, and benzo[a]pyrene (B[a]P). The dearth of...
The farnesoid X receptor (FXR) regulates bile acid, lipid and glucose metabolism. Here we
show that treatment of mice with glycine-b-muricholic acid (Gly-MCA) inhibits FXR signalling
exclusively in intestine, and improves metabolic parameters in mouse models of obesity.
Gly-MCA is a selective high-affinity FXR inhibitor that can be administered orally...
Full Text:
mice.
(f, g) Glucose tolerance test (f) and the area under the curve (AUC) (g) in vehicle- and Gly-MCA
The farnesoid X receptor (FXR) regulates bile acid, lipid and glucose metabolism. Here we
show that treatment of mice with glycine-b-muricholic acid (Gly-MCA) inhibits FXR signalling
exclusively in intestine, and improves metabolic parameters in mouse models of obesity.
Gly-MCA is a selective high-affinity FXR inhibitor that can be administered orally...
Full Text:
, Kristopher W. Krausz1, Jingmin Shi1, Chad N. Brocker1,
Dhimant Desai4, ShantuG. Amin4, William H. Bisson5
The farnesoid X receptor (FXR) regulates bile acid, lipid and glucose metabolism. Here we show that treatment of mice with glycine-β-muricholic acid (Gly-MCA) inhibits FXR signalling exclusively in intestine, and improves metabolic parameters in mouse models of obesity. Gly-MCA is a selective high-affinity FXR inhibitor that can be administered orally...
The farnesoid X receptor (FXR) regulates bile acid, lipid and glucose metabolism. Here we show that treatment of mice with glycine-b-muricholic acid (Gly-MCA) inhibits FXR signalling exclusively in intestine, and improves metabolic parameters in mouse models of obesity. Gly-MCA is a selective high-affinity FXR inhibitor that can be administered orally...