No abstract

This review depicts in vitro and in vivo results obtained with nucleotide prodrugs (pronucleotides) bearing S-acyl-2-thioethyl (SATE) groups as esterase-labile phosphate protections. New developments are illustrated by the design of mononucleoside mixed phosphoester derivatives leading to the selective intracellular delivery of the corresponding 5'-mononucleotide through two different enzyme-mediated activation steps.

No abstract

through in vitro selection with 3TC or FTC (11,12,23). DNA sequence analysis of the RT gene amplified from a patient who had received 3TC therapy for 4 months revealed a mixture of the mutation at codon 184 from Met to Val (M184V) and the parental genotype, indicating that the mutation at the methionine at codon 184 (Met-184) can occur in vivo (23). In order to understand the mechanisms of action and drug resistance, the 5'-triphosphates of L-ddC (L-ddCTP) and L-FddC (LFddCTP) were synthesized, and the inhibitory effects of these triphosphate derivatives toward HIV-1 RT recombinant wildtype (WT) (WT RT) and the site-directed mutagenesis recom-