Mutation of a single amino acid of pregnane X receptor switches an antagonist to agonist by altering AF-2 helix positioning
Andrew D. Huber, William C. Wright, Wenwei Lin, Kinjal Majumder, Jonathan Low, Jing Wu, Cameron D. Buchman, David J. Pintel, Taosheng Chen
Topics & Concepts
Pregnane X receptorAgonistAntagonistChemistryReceptorPharmacologyLigand (biochemistry)G protein-coupled receptorPartial agonistBiophysicsStereochemistryBiochemistryBiologyNuclear receptorTranscription factorGenePharmacogenetics and Drug MetabolismReceptor Mechanisms and SignalingHormonal Regulation and Hypertension