Bile acids (BAs) are considered signaling molecules able to interact with nuclear and membrane endogenous receptors, inducing several cellular networks that regulate lipids, glucose and bile acids homeostasis. Two well-known targets of BAs are the endogenous nuclear receptor FXR (farnesoid-x-receptor) and the membrane receptor GPBAR1 (G-protein coupled receptor 1) and since their activation is linked to the control of different metabolic and enterohepatic functions, they could be considered efficient targets in the treatment of several human diseases. In the last few years, medicinal chemistry modifications on bile acid scaffolds, afforded a large amount of exogenous derivatives with different pharmacological profiles, useful in the treatment of metabolic and enterohepatic disorders, ranging from metabolic syndrome, diabetes, cholestasis and non-alcoholic steatohepatiti
