NLM AIDSLINE An in situ pig liver esterase assay as a useful predictive tool for the
likely in vitro anti viral activity of phosphoramidate pro-drugs.
Ballatore C; McGuigan C; De Clercq E; Balzarini J; Welsh School of
October 30, 1999
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