Recent Developments of Peptidomimetic HIV-1 Protease Inhibitors

Title: Recent Developments of Peptidomimetic HIV-1 Protease Inhibitors

Volume: 18 Issue: 29

Author(s): X. Qiu and Z.-P. Liu

Affiliation:

Keywords: Antiviral, drug-resistance, human immunodeficiency virus, HIV, ligands, multidrug-resistant, mutant HIV-1 variants, protease, inhibitors, peptidomimetic, substrate-based drug design, substrate-envelope hypothesis, protease inhibitors

Abstract: HIV protease plays a crucial role in the viral life cycle by processing the viral Gag and Gag-Pol polyproteins into structural and functional proteins essential for viral maturation. Inhibition of HIV-1 protease leads to the production of noninfectious virus particles and hence is an important therapeutic target for antiviral therapy in AIDS patients. Among many strategies to combat this disease, highly active antiretroviral therapy (HAART) with HIV protease inhibitors (PIs) in combination with reverse transcriptase inhibitors and fusion inhibitor continues to be the first line treatment for control of HIV infection. However, the rapid emergence of drug-resistant HIV-1 strains and the appearance of cross-resistance are severely limiting the long-term treatment options. Thus, numerous efforts have been made in the design and synthesis of novel protease inhibitors with broad-spectrum activity against multidrug-resistant HIV-1 variants by medicinal chemists. This review will focus on the substrate-based drug design of novel peptidomimetic PIs in recent years since 2006.

Cite this article as:

Qiu X. and Liu Z.-P., Recent Developments of Peptidomimetic HIV-1 Protease Inhibitors, Current Medicinal Chemistry 2011; 18 (29) . https://dx.doi.org/10.2174/092986711797287566