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Purpose of review: TGR5 (Gpbar-1) is an emerging drug target for metabolic, intestinal and liver diseases. In liver, the highest expression of TGR5 is found in biliary epithelial cells. This review focusses on the function of TGR5 in cholangiocytes and the potential role of the receptor in biliary diseases.

Recent findings: TGR5 is localized in the primary cilium and the apical membrane domain of cholangiocytes, where the receptor exerts secretory, proliferative and antiapoptotic effects. Recent human and animal studies using bile acid analogues suggest a therapeutic potential for TGR5 in primary biliary cirrhosis but not in primary sclerosing cholangitis.

Summary: TGR5 has protective functions in cholangiocytes. Further studies are needed to determine the therapeutic potential of TGR5 agonists and antagonists in biliary diseases.

(C) 2013 Lippincott Williams & Wilkins, Inc.