Development of a New Type of Protease Inhibitors, Efficacious against FIV and HIV Variants

Based on the structural analysis of FIV protease and drug-resistant HIV proteases and molecular modeling, a new type of inhibitors with a small P3 residue has been developed. These inhibitors are effective against HIV and its drug-resistant mutants, as well as SIV and FIV. Modification of existing H...

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Published inJournal of the American Chemical Society Vol. 121; no. 6; pp. 1145 - 1155
Main Authors Lee, Taekyu, Le, Van-Duc, Lim, Dongyeol, Lin, Ying-Chuan, Morris, Garrett M, Wong, Andrew L, Olson, Arthur J, Elder, John H, Wong, Chi-Huey
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 17.02.1999
Amer Chemical Soc
Subjects
Chemistry
Chemistry, Multidisciplinary
Feline immunodeficiency virus
Human immunodeficiency virus
Physical Sciences
Science & Technology
DESIGN
MUTANTS
FELINE IMMUNODEFICIENCY VIRUS
IDENTIFICATION
PROTEINASE
ESCAPE
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Summary:Based on the structural analysis of FIV protease and drug-resistant HIV proteases and molecular modeling, a new type of inhibitors with a small P3 residue has been developed. These inhibitors are effective against HIV and its drug-resistant mutants, as well as SIV and FIV. Modification of existing HIV protease inhibitors by reducing the size of the P3 residue has the same effect. This finding provides a new strategy for the development of HIV protease inhibitors effective against the wild-type and drug-resistant mutants. It further supports the use of FIV protease as a useful model for drug-resistant HIV proteases, which often have a more constricted binding region for the P3 group or the combined P3 and P1 groups.
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ISSN:0002-7863
1520-5126
DOI:10.1021/ja982893p