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Rational Design of Peptide-Based HIV Proteinase Inhibitors
Abstract
A series of peptide derivatives based on the transition-state mimetic concept has been designed that inhibit the proteinase from the human immunodeficiency virus (HIV). The more active compounds inhibit both HIV-1 and HIV-2 proteinases in the nanomolar range with little effect at 10 micromolar against the structurally related human aspartic proteinases. Proteolytic cleavage of the HIV-1 gag polyprotein (p55) to the viral structural protein p24 was inhibited in chronically infected CEM cells. Antiviral activity was observed in the nanomolar range (with one compound active below 10 nanomolar) in three different cell systems, as assessed by p24 antigen and syncytium formation. Cytotoxicity was not detected at 10 and 5 micromolar in C8166 and JM cells, respectively, indicating a high therapeutic index for this new class of HIV proteinase inhibitors.
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Cited by
INHIBITORS OF HIV-1 PROTEASE: A Major Success of Structure-Assisted Drug Design
Wlodawer, A., & Vondrasek, J. (1998) · Annual Review of Biophysics and Biomolecular Structure · doi:10.1146/annurev.biophys.27.1.249 · Cited by 734
Jaskolski, M., Tomasselli, A. G., Sawyer, T. K., Staples, D. G., Heinrikson, R. L., Schneider, J., Kent, S. B. H., & Wlodawer, A. (1991) · Biochemistry · doi:10.1021/bi00220a023 · Cited by 227
Smith, A. J. T., Zhang, X., Leach, A. G., & Houk, K. N. (2009) · Journal of Medicinal Chemistry · doi:10.1021/jm800498e · Cited by 193
Beyond reverse transcription: molecular mechanisms and emerging paradigms in retroviral replication
Jehad, M. A., Ali, L. M., Pillai, V. N., Prabhu, S. G., Mustafa, F., & Rizvi, T. A. (2026) · FEMS Microbiology Reviews · doi:10.1093/femsre/fuaf066 · Cited by 5
“…PR coding domain or inhibition of PR activity result in virions containing unprocessed Gag, rendering them noninfectious (Craw-ford and Goff 1985 , Katoh et al. 1985 , Kohl et al. 1988 , Ashorn et al. 1990 , Meek et al. 1990 , Roberts et al. 1990 , Stewart et al. 1990 , Sommerfelt et al. 1992 ).”
Metadata
- Authors
- Roberts, N. A., Martin, J. A., Kinchington, D., Broadhurst, A. V., Craig, J. C., Duncan, I. B., Galpin, S. A., Handa, B. K., Kay, J., Kröhn, A., Lambert, R. W., Merrett, J. H., Mills, J. S., Parkes, K. E. B., Redshaw, S., Ritchie, A. J., Taylor, D. L., Thomas, G. J., & Machin, P. J.
- Venue
- Science
- Published
- 1990-04-20
- Volume
- 248
- Issue
- 4953
- Pages
- 358-361
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W1966952510
- Cited by
- 929
- References
- 0
- FWCI
- 60.78
- Type
- journal article
- Language
- en
- Open access
- closed
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- Roberts, N. A., Martin, J. A., Kinchington, D., Broadhurst, A. V., Craig, J. C., Duncan, I. B., Galpin, S. A., Handa, B. K., Kay, J., Kröhn, A., Lambert, R. W., Merrett, J. H., Mills, J. S., Parkes, K. E. B., Redshaw, S., Ritchie, A. J., Taylor, D. L., Thomas, G. J., & Machin, P. J. (1990). Rational Design of Peptide-Based HIV Proteinase Inhibitors. Science. https://doi.org/10.1126/science.2183354
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