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 in | Journal of the American Chemical Society Vol. 121; no. 6; pp. 1145 - 1155 |
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| Main Authors | , , , , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
WASHINGTON
American Chemical Society
17.02.1999
Amer Chemical Soc |
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| Abstract | 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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| AbstractList | 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. |
| Author | Lin, Ying-Chuan Morris, Garrett M Le, Van-Duc Wong, Andrew L Olson, Arthur J Lee, Taekyu Wong, Chi-Huey Elder, John H Lim, Dongyeol |
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| Keywords | DESIGN MUTANTS FELINE IMMUNODEFICIENCY VIRUS IDENTIFICATION PROTEINASE ESCAPE |
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| Snippet | 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... |
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| SubjectTerms | Chemistry Chemistry, Multidisciplinary Feline immunodeficiency virus Human immunodeficiency virus Physical Sciences Science & Technology |
| Title | Development of a New Type of Protease Inhibitors, Efficacious against FIV and HIV Variants |
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