Article
Derivatives of mesoxalic acid block translocation of HIV-1 reverse transcriptase.
The Journal of biological chemistry - 16 Jan 2015
Bernatchez Jean A, Paul Rakesh, Tchesnokov Egor P, Ngure Marianne, Beilhartz Greg L, Berghuis Albert M, Lavoie Rico, Li Lianhai, Auger Anick, Melnyk Roman A, Grobler Jay A, Miller Michael D, Hazuda Daria J, Hecht Sidney M, Götte Matthias
Abstract excerpt
The pyrophosphate mimic and broad spectrum antiviral phosphonoformic acid (PFA, foscarnet) was shown to freeze the pre-translocational state of the reverse transcriptase (RT) complex of the human immunodeficiency virus type 1 (HIV-1). However, PFA lacks a specificity domain, which is seen as a major reason for toxic side effects associated with the clinical use of this drug. Here, we studied the mechanism of...
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