FXR Agonists: From Bench to Bedside, a Guide for Clinicians

Excerpt

Farnesoid X receptors (FXRs) belong to a superfamily of receptors known as the nuclear hormone receptors [1]. Nuclear hormone receptors are ligand-activated transcription factors that regulate key functions including cell differentiation, several metabolic pathways such as insulin signaling, cholesterol homeostasis, and bile acid metabolism [2]. These receptors have highly conserved DNA- and ligand-binding domains, and depending on their DNA-binding properties, they are further subclassified into different subcategory receptors including farnesoid X receptors (FXRs). These receptors are highly expressed in tissues that are involved in bile acid (BA) metabolism such as liver and intestines, and they are also present in kidney and to a lower extent in adipose tissue [3]. They are responsible for modulating BA homeostasis by regulating genes involved in BA synthesis, secretion, conjugation, transportation, absorption, and detoxification [4]. …