Resistance to the Anti-Human Immunodeficiency Virus Type 1 Compound l-Chicoric Acid Results from a Single Mutation at Amino Acid 140 of Integrase
AUTOR(ES)
King, Peter J.
FONTE
American Society for Microbiology
RESUMO
l-Chicoric acid is an inhibitor of human immunodeficiency virus type 1 (HIV-1) integrase in vitro and of HIV-1 replication in tissue culture. Following 3 months of selection in the presence of increasing concentrations of l-chicoric acid, HIV-1 was completely resistant to the compound. Introduction of the mutant integrase containing a single glycine-to-serine amino acid change at position 140 into the native, l-chicoric acid-sensitive virus demonstrated that this change was sufficient to confer resistance to l-chicoric acid. These results confirm through natural selection previous biochemical studies showing that l-chicoric acid inhibits integrase and that the drug is likely to interact at residues near the catalytic triad in the integrase active site.
ACESSO AO ARTIGO
http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=110234Documentos Relacionados
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