Antiviral properties of Ro 31-8959, an inhibitor of human immunodeficiency virus (HIV) proteinase.

Abstract

Ro 31-8959 inhibits the spread of HIV infection and the production of cytopathic effects in cultures of acutely infected cells. IC50 values for these effects are in the range 0.5-6.0 nM and IC90 values are in the range 6.0-30.0 nM. This inhibitor is effective even when added to cultures at a late stage of infection, after syncytia have started to form. Virus antigen, virus particles and virus cytopathic effects can largely be cleared from cultures treated with compound from 3 days until 6 days post infection. In chronically-infected cells, inhibition of virus maturation can be detected after 24 hours' treatment with 10 nM Ro 31-8959. In addition, a significant reduction of the proteolytic processing of p56 to p24 can be demonstrated in these cells with compound at picomolar concentrations. These properties indicate that Ro 31-8959 is highly effective against HIV with the potential to inhibit acute, established acute and chronic infections.

• Authors: J C Craig, I B Duncan, D Hockley, C Grief, N A Roberts, J S Mills
• Journal: Antiviral research (Antiviral Res) Vol. 16 Issue 4 Pg. 295-305 (Dec 1991) ISSN: 0166-3542 [Print] Netherlands
• PMID: 1810306 (Publication Type: Journal Article)

Chemical References

• Antiviral Agents
• HIV Antigens
• HIV Protease Inhibitors
• HIV Protease
• Saquinavir

Topics

• Antiviral Agents (pharmacology)
• Cell Fusion (drug effects)
• Cells, Cultured
• HIV Antigens (analysis)
• HIV Infections (drug therapy)
• HIV Protease (pharmacology)
• HIV Protease Inhibitors
• Humans
• In Vitro Techniques
• Saquinavir
• Time Factors
• Virus Replication (drug effects)