Bile acid receptors and the kidney.

Bile acids act as activating signals of endogenous renal receptors: the nuclear receptor farnesoid X receptor (FXR) and the membrane-bound G protein-coupled bile acid receptor 1 (GPBAR1, also known as TGR5). In recent years, bile acids have emerged as important for renal pathophysiology by activating FXR and TGR5 and transcription factors relevant for lipid, cholesterol and carbohydrate metabolism, as well as genes involved in inflammation and renal fibrosis.

Activation of bile acid receptors has a promising therapeutic potential in prevention of diabetic nephropathy and obesity-induced renal damage, as well as in nephrosclerosis. During the past decade, progress has been made in understanding the biology and mechanisms of bile acid receptors in the kidney and in the development of specific bile acid receptor agonists.

In this review, we discuss current knowledge on the roles of FXR and TGR5 in the physiology of the kidney and the latest advances made in development and characterization of bile acid analogues that activate bile acid receptors for treatment of renal disease.