Screening of Potential HIV-1 Inhibitors/Replication Blockers Using Secure Lentiviral in Vitro System

Acta Naturae. 2011 Oct;3(4):55-65.

Abstract

The development and usage of safe cell systems for testing agents which possess anti-HIV activity is a very important factor in the design of new drugs. We have described in detail a system we designed that is based on lentiviral vectors (Prokofjeva et. al.,Antiviral Therapy,in print) for swift and completely safe screening of potential HIV-1 replication inhibitors. The system enables one to test the efficiency of the inhibitory activity of compounds whose action is directed towards either wild-type HIV-1 reverse transcriptase or integrase, or mutant enzymes corresponding to the drug-resistant virus form. Testing results of a number of already known drugs, which correlate well with published data as well as data on newly synthesized compounds, were obtained. Application of this system substantially broadens the possibilities of preclinical anti-HIV drugs testing.

Keywords: HIV; lentiviral vectors; non-nucleoside reverse transcriptase inhibitors; integrase inhibitors; nucleoside reverse transcriptase inhibitors; pseudo-HIV-1 particles.