How to modulate FXR activity to treat the Metabolic Syndrome

Abstract

The Metabolic Syndrome (MS) represents a public health problem which takes epidemic proportions worldwide. In addition to life-style interventions the development of effective therapies for the MS and its complications such as cardiovascular disease (CVD) and type 2 diabetes (T2D) is a major challenge of the future decades. The nuclear receptor farnesoid X receptor (FXR) is a potential pharmacological target, because of its broad spectrum of functions and the possibility of modulating its activity in a gene-specific manner by the so-called selective bile acid receptor modulators (SBARM). This review will discuss the numerous regulatory functions of FXR that overlap with components of the MS and the potential benefit of modulating FXR activity for MS therapy.