Document 0644 DOCN M94A0644 TI In vitro activity of protease inhibitors against HIV. DT 9412 AU Birch C; Tachedjian G; Tyssen D; Grobelny D; Virology Department, NCHVR, Fairfield, Victoria. SO Annu Conf Australas Soc HIV Med. 1993 Oct 28-30;5:62 (abstract no. TB2). Unique Identifier : AIDSLINE ASHM5/94349011 AB HIV encodes a novel aspartyl protease that represents an important virus-specific target for inhibitors. We have been studying a series of transition state analogue inhibitors designed and synthesised in Australia that have potent and specific activity against HIV replication in cell culture. (Note: the structure of these compounds will not be presented). The inhibitors are active against HIV-1 and HIV-2 in acutely and chronically infected cells, working through a mechanism involving inhibition of cleavage of p55 to its structural components. As a result, virions produced in the presence of these drugs are noninfectious. The inhibitors are also active against AZT-resistant HIV and the simian immunodeficiency virus, but fail to inhibit feline immunodeficiency virus. These results will be presented, along with preliminary details on the pharmacokinetics of selected inhibitors. DE Antiviral Agents/*PHARMACOLOGY Cells, Cultured Gene Products, gag/ANTAGONISTS & INHIB Human HIV Protease Inhibitors/*PHARMACOLOGY HIV-1/*DRUG EFFECTS HIV-2/*DRUG EFFECTS Protein Precursors/ANTAGONISTS & INHIB Virus Replication/*DRUG EFFECTS MEETING ABSTRACT SOURCE: National Library of Medicine. NOTICE: This material may be protected by Copyright Law (Title 17, U.S.Code).