Title : Activation of the antiviral prodrug oseltamivir is impaired by two newly identified carboxylesterase 1 variants.

Pub. Date : 2009 Feb

PMID : 19022936






6 Functional Relationships(s)
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1 Activation of the antiviral prodrug oseltamivir is impaired by two newly identified carboxylesterase 1 variants. Oseltamivir carboxylesterase 1 Homo sapiens
2 The conversion of oseltamivir to its active metabolite oseltamivir carboxylate is dependent on ester hydrolysis mediated by carboxylesterase 1 (CES1). Oseltamivir carboxylesterase 1 Homo sapiens
3 The conversion of oseltamivir to its active metabolite oseltamivir carboxylate is dependent on ester hydrolysis mediated by carboxylesterase 1 (CES1). Oseltamivir carboxylesterase 1 Homo sapiens
4 The aim of the present study was to investigate the function of these mutations on activating (hydrolyzing) oseltamivir to oseltamivir carboxylate using the cell lines expressing wild type (WT) and each mutant CES1. Oseltamivir carboxylesterase 1 Homo sapiens
5 In vitro incubation studies demonstrated that the S9 fractions prepared from the cells transfected with WT CES1 and human liver tissues rapidly convert oseltamivir to oseltamivir carboxylate. Oseltamivir carboxylesterase 1 Homo sapiens
6 These results suggest that the therapeutic efficacy of oseltamivir could be compromised in treated patients expressing either functional CES1 mutation. Oseltamivir carboxylesterase 1 Homo sapiens