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Journal Article
Bile acid receptors as targets for drug development
2014
Overview
Key Points
The discovery of dedicated bile acid receptors and further research defined multiple bile acid signalling routes affecting bile acid synthesis, lipid synthesis, gluconeogenesis, inflammation, liver fibrosis and cancer
Steroidal and nonsteroidal agonists of bile acid receptors have been developed as potential treatments for cholestatic and metabolic liver diseases, including primary biliary cirrhosis, primary sclerosing cholangitis and NASH
Randomized, placebo-controlled clinical trials for the treatment of primary biliary cirrhosis and NASH with the farnesoid X receptor (FXR) agonist obeticholic acid are the first clinical trials initiated
Future indications for FXR and TGR5 agonists include genetic cholestatic syndromes, intrahepatic cholestasis of pregnancy, atherosclerosis, IBS, bile-reflux oesophagitis, IBD, hepatocellular and colon carcinoma
Bile acids have a crucial role in the digestion of dietary lipids and as signalling molecules in a number of metabolic pathways. Bile acid receptors have become attractive therapeutic targets for liver disease and metabolic disorders. Here, the authors provide an overview of bile acid signalling in humans and highlight the therapeutic potential of compounds that target these pathways.
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 signalling cascades. These cascades affect the expression of a great number of target genes relevant for bile acid, cholesterol, lipid and carbohydrate metabolism, as well as genes involved in inflammation, fibrosis and carcinogenesis. Pregnane X receptor, vitamin D receptor and constitutive androstane receptor are additional nuclear receptors that respond to bile acids, albeit to a more restricted set of species of bile acids. Recognition of dedicated bile acid receptors prompted the development of semi-synthetic bile acid analogues and nonsteroidal compounds that target these receptors. These agents hold promise to become a new class of drugs for the treatment of chronic liver disease, hepatocellular cancer and extrahepatic inflammatory and metabolic diseases. This Review discusses the relevant bile acid receptors, the new drugs that target bile acid signalling and their possible applications.
Publisher
Nature Publishing Group UK,Nature Publishing Group
