The inhibitory activity of a peptide derivative against the growth of simian immunodeficiency virus in C8166 cells.
The peptide derivative Ro 31-8959 is a potent and selective inhibitor of the aspartic proteinases encoded by HIV-1 and HIV-2 and it arrests the growth of both viruses in cell culture. We have demonstrated similar effects against the simian immunodeficiency virus SIVmac251 in the human T-cell line, C8166 (ED50 = 6nM) with a therapeutic index of 4,500. The antiviral activity of Ro 31-8959 was 250 and 22 times greater than that of ddI and ddC, respectively. The mode of action was confirmed by accumulation of the polyprotein p55 with concomitant reduction of the cleavage product, p27, and by the production of immature virions.
Martin
J A
JA
Research Centre, Roche Products Ltd., Welwyn Garden City, Herts, UK.
Mobberley
M A
MA
Redshaw
S
S
Burke
A
A
Tyms
A S
AS
Ryder
T A
TA
D000818:Animals; D000998:Antiviral Agents / Q000494:pharmacology*; D002460:Cell Line; D016049:Didanosine / Q000494:pharmacology; D016333:HIV Protease / Q000494:pharmacology; D017320:HIV Protease Inhibitors; D006801:Humans; D008854:Microscopy, Electron; D019258:Saquinavir; D015302:Simian Immunodeficiency Virus / Q000187:drug effects / Q000254:growth & development* / Q000648:ultrastructure; D016047:Zalcitabine / Q000494:pharmacology
D000998:Antiviral Agents; D017320:HIV Protease Inhibitors; D016047:Zalcitabine; D016333:HIV Protease; D016049:Didanosine; D019258:Saquinavir