Asymmetric Deactivation of HIV-1 gp41 following Fusion Inhibitor Binding
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چکیده
منابع مشابه
Asymmetric Deactivation of HIV-1 gp41 following Fusion Inhibitor Binding
Both equilibrium and nonequilibrium factors influence the efficacy of pharmaceutical agents that target intermediate states of biochemical reactions. We explored the intermediate state inhibition of gp41, part of the HIV-1 envelope glycoprotein complex (Env) that promotes viral entry through membrane fusion. This process involves a series of gp41 conformational changes coordinated by Env intera...
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The HIV-1 envelope glycoprotein (Env) gp41 plays a crucial role in the viral fusion process. The peptides derived from the C-terminal heptad repeat (CHR) of gp41 are potent HIV fusion inhibitors. However, the activity of these anti-HIV-1 peptides in vivo may be attenuated by their induction of anti-gp41 antibodies. Thus, it is essential to identify antiviral peptides or proteins with low, or no...
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A variety of molecules in human blood have been implicated in the inhibition of HIV-1. However, it remained elusive which circulating natural compounds are most effective in controlling viral replication in vivo. To identify natural HIV-1 inhibitors we screened a comprehensive peptide library generated from human hemofiltrate. The most potent fraction contained a 20-residue peptide, designated ...
متن کاملDesign of a highly potent HIV-1 fusion inhibitor targeting the gp41 pocket.
OBJECTIVE T20 (Enfuvirtide), which is a 36-residue peptide derived from the C-terminal heptad repeat (CHR) of gp41, is the only clinically available HIV-1 fusion inhibitor, but it easily induces drug resistance, which calls for next-generation drugs. DESIGN We recently demonstrated that the M-T hook structure can be used to design a short CHR peptide that specifically targets the conserved gp...
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A novel chimeric protein-based HIV-1 fusion inhibitor targeting gp41 with high potency and stability Chungen Pan, Lifeng Cai, Hong Lu, Lu Lu, and Shibo Jiang* From Lindsley F. Kimball Research Institute, New York Blood Center, New York, NY 10065 MOE/MOH Key Laboratory of Medical Molecular Virology and Institute of Biomedical Sciences, Shanghai Medical College, Fudan University, Shanghai 200032,...
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ژورنال
عنوان ژورنال: PLoS Pathogens
سال: 2009
ISSN: 1553-7374
DOI: 10.1371/journal.ppat.1000674