Novel antagonists reveal the mechanism of PXR inhibition

Abstract

The pregnane X receptor (PXR) is a key regulator of metabolism, but the mechanisms underlying its antagonism remain unclear. Garcia-Maldonado et al. reported potent new antagonists and their co-crystal structures, revealing molecular determinants of PXR antagonism and paving the way for developing antagonists as therapeutics and preventing undesirable PXR activation.

Keywords: PXR; antagonist; crystal structures; drug discovery.