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Novel antagonists reveal the mechanism of PXR inhibition

R. Kamaraj, P. Pavek

. 2024 ; 45 (11) : 961-963. [pub] 20241016

Language English Country England, Great Britain

Document type Journal Article

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.

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