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Stereospecific Metabolism of Itraconazole by CYP3A4: Dioxolane Ring Scission of Azole Antifungals

Itraconazole (ITZ) is a mixture of four cis-stereoisomers that inhibit CYP3A4 potently and coordinate CYP3A4 heme via the triazole nitrogen. However, (2R,4S,2′R)-ITZ and (2R,4S,2′S)-ITZ also undergo stereoselective sequential metabolism by CYP3A4 at a site distant from the triazole ring to 3′-OH-ITZ...

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Detalhes bibliográficos
Main Authors: Peng, Chi-Chi, Shi, Wei, Lutz, Justin D., Kunze, Kent L., Liu, Jun O., Nelson, Wendel L., Isoherranen, Nina
Formato: Artigo
Idioma:Inglês
Publicado em: The American Society for Pharmacology and Experimental Therapeutics 2012
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3286268/
https://ncbi.nlm.nih.gov/pubmed/22106171
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1124/dmd.111.042739
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