Probing ligand structure-activity relationships in pregnane X receptor (PXR): efavirenz and 8-hydroxyefavirenz exhibit divergence in activation

Efavirenz (EFV), an antiretroviral that interacts clinically with co-administered drugs via activation of the pregnane X receptor (PXR), is extensively metabolized by the cytochromes P450. We tested whether its primary metabolite, 8-hydroxyEFV (8-OHEFV) can activate PXR and potentially contribute to...

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Detalhes bibliográficos
Publicado no:ChemMedChem
Main Authors: Narayanan, Bhargavi, Lade, Julie M., Heck, Carley J.S., Dietz, Kevin D., Wade, Herschel, Bumpus, Namandjé N.
Formato: Artigo
Idioma:Inglês
Publicado em: 2018
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6081956/
https://ncbi.nlm.nih.gov/pubmed/29430850
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1002/cmdc.201700730
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