Recent advances have provided important new information on the physiol
ogical mechanisms of bile acid transport and metabolism. Bile acids, w
hich are essential for the digestion and absorption of lipids and lipi
d-soluble vitamins, are metabolic: products of cholesterol and are a m
ajor regulator of cholesterol homeostasis. Bile acids are pharmacologi
cally interesting as potential carriers of liver-specific drugs, absor
ption enhancers and as new cholesterol-lowering agents. Furthermore, t
he tools of molecular recognition and combinatorial chemistry have bee
n used to explore the drug discovery possibilities of bile acids. The
authors explore current understanding and future prospects for bile ac
id research.