Farnesoid X receptor in human malignancies: an overview

Abstract

Cancer represents a leading cause of death in developed and developing countries, accounting for 8.8 million deaths in 2015. These numbers are expected to continue rising with 13.1 million deaths estimated in 2030. Although the earlier diagnosis and increasing treatment options have improved the survival rates for the majority of cancers, many tumors exhibit therapeutic resistance and severe adverse effects remain major therapeutic hurdles. Thus, the main challenge of the cancer research area is the definition of additional treatment options tailored on the distinct tumor characteristics and the expression of appropriate targets. Nuclear receptors, controlling many biological features of cancers as proliferation, survival, apoptosis, and differentiation, possess a significant clinical relevance in disease management, representing a “druggable” class of molecules useful for potential therapeutic intervention. In the last years, among the nuclear receptors, the metabolic sensor Farnesoid X Receptor was recognized to play a role in carcinogenesis, acting either as an oncogene or as a tumor suppressor gene. Here, we will summarize the current knowledge on the FXR role in human cancers, highlighting its ligands as new potential anticancer tools.