Nuclear bile acid receptor FXR as pharmacological target: are we there yet?
The farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily that is primarily expressed in the enterohepatic system where it functions as intracellular sensor for bile acids. Ligand dependent FXR activation induces transcriptional responses to coordinately regulate bile acid, cholesterol, triglyceride and glucose metabolism, and to protect the intestinal mucosa from bacterial overgrowth and inflammatory insults. Here we discuss the latest discoveries in FXR-driven metabolic pathways with relevance to pathophysiology and novel therapeutic approaches of several conditions such as hypertriglyceridemia, type 2 diabetes, cholesterol gallstone disease, steato-hepatitis and metabolic syndrome.
Modica
Salvatore
S
Department of Cell Biology and Oncology, Consorzio Mario Negri Sud, Via Nazionale 8A, Santa Maria Imbaro Chieti, CH, Chieti 66030, Italy.
Moschetta
Antonio
A
D000818:Animals; D001647:Bile Acids and Salts / Q000378:metabolism*; D005947:Glucose / Q000378:metabolism; D006801:Humans; D007413:Intestinal Mucosa / Q000378:metabolism; D050356:Lipid Metabolism; D008107:Liver Diseases / Q000188:drug therapy* / Q000378:metabolism*; D018160:Receptors, Cytoplasmic and Nuclear / Q000378:metabolism*
D001647:Bile Acids and Salts; D018160:Receptors, Cytoplasmic and Nuclear; D005947:Glucose