Impact of Nuclear Receptors CAR, PXR, FXR, and VDR, and Their Ligands On Enzymes and Transporters

Abstract

Nuclear receptors play a central role on the mechanism of inductiontype drug-drug interactions by acting as xenosensing transcription factors. Together, PXR, CAR, FXR, and VDR form a core group of nuclear receptors that regulate the expression of a number of important drug-metabolizing enzymes and drug transporters. In this chapter, the molecular determinants of adaptive response to drug exposure are detailed in the context of clinical relevance and drug development.