Title:Advances in Non-peptidomimetic HIV Protease Inhibitors
VOLUME: 21 ISSUE: 17
Author(s):X. Pang, Z. Liu and G. Zhai
Affiliation:Department of Pharmaceutics, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.
Keywords:Antiviral, drug-resistance, human immunodeficiency virus, non-peptidomimetic inhibitors, protease inhibitors.
Abstract:HIV protease plays a crucial role in the viral life cycle. It can cleave a series of heptamers in the viral Gag and
GagPol precursor proteins to generate mature infectious virus particles. Successful inhibition of the protease will prevent
this maturation step and hence block the spreading of HIV. However, the rapid emergence of drug resistance makes it urgent
to develop new HIV protease inhibitors to combat the global disease. Besides, poor oral bioavailability, unacceptable
side effects, high treatment cost and pill burden also trouble the application of HIV protease inhibitors. In such situations,
non-peptidomimetic HIV protease inhibitors have drawn an increasing interest as a potential therapeutic option due to
their small molecular weight, favorable bioavailability, high stability in vivo, low resistance and cost of production. In this
review, we present the recent advances in non-peptidomimetic HIV protease inhibitors. Their design strategies, biological
activities, resistance profiles, as well as clinical application will also be discussed.
