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An in situ pig liver esterase assay as a useful predictive tool for the likely in vitro anti viral activity of phosphoramidate pro-drugs.


Nucleosides Nucleotides. 1999 Apr-May;18(4-5):967-9. Unique Identifier :

The pig liver esterase (PLE) assay has been designed to "reproduce" in vitro the first step of the metabolism of phosphoramidate pro-drugs that generates the free amino acyl phosphoramidate intermediate which has been described as a key metabolite necessary but not sufficient for the biological activity. The method could be used as a predictive tool for the likely in vitro biological activity as well as for Structure-Activity Relationship establishment (SAR).

JOURNAL ARTICLE Animal Anti-HIV Agents/CHEMISTRY/*PHARMACOLOGY Cell Line Esterases/*METABOLISM Human Liver/*ENZYMOLOGY Nuclear Magnetic Resonance Organophosphorus Compounds/CHEMISTRY/*PHARMACOLOGY Prodrugs/CHEMISTRY/*PHARMACOLOGY Structure-Activity Relationship Swine


Information in this article was accurate in October 30, 1999. The state of the art may have changed since the publication date. This material is designed to support, not replace, the relationship that exists between you and your doctor. Always discuss treatment options with a doctor who specializes in treating HIV.