Anti-HIV activity of (-)-(2R,4R)-1- (2-hydroxymethyl-1,3-dioxolan-4-yl)-thymine against drug-resistant HIV-1 mutants and studies of its molecular mechanism.

doi:10.1021/jm050060l

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Article

Anti-HIV activity of (-)-(2R,4R)-1- (2-hydroxymethyl-1,3-dioxolan-4-yl)-thymine against drug-resistant HIV-1 mutants and studies of its molecular mechanism.

Journal of medicinal chemistry - 16 Jun 2005

Chu Chung K, Yadav Vikas, Chong Youhoon H, Schinazi Raymond F

Abstract excerpt

(-)-(2R,4R)-1-(2-Hydroxymethyl-1,3-dioxolan-4-yl)thymine (DOT) is the first thymidine kinase-activated nucleoside that is significantly active against all of the clinically significant NRTI-resistant HIV-1 mutants, including AZT (D67N/K70R/T215Y/K219Q), Tenofovir (K65R), and Lamivudine (M184V). To understand the molecular mechanism of drug resistance and the antiviral activity of DOT against drug-resistant RTs,...

Topics

Anti-HIV Agents
Binding Sites
Drug Resistance, Viral
HIV Reverse Transcriptase
HIV-1
Models, Molecular
Mutation
Reverse Transcriptase Inhibitors
Stereoisomerism

Source

Open in PubMed

Identifiers

PMID: 15943470
DOI: 10.1021/jm050060l

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