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Review
. 2015 Apr 8:7:95-104.
doi: 10.2147/HIV.S79956. eCollection 2015.

HIV protease inhibitors: a review of molecular selectivity and toxicity

Zhengtong Lv  1 , Yuan Chu  1 , Yong Wang  1
Affiliations
Review

HIV protease inhibitors: a review of molecular selectivity and toxicity

Zhengtong Lv et al. HIV AIDS (Auckl). .

Abstract

Highly active antiretroviral therapy (HAART) is recognized as the most effective treatment method for AIDS, and protease inhibitors play a very important role in HAART. However, poor bioavailability and unbearable toxicity are their common disadvantages. Thus, the development of safer and potentially promising protease inhibitors is eagerly needed. In this review, we introduced the chemical characteristics and associated side effects of HIV protease inhibitors, as well as the possible off-target mechanisms causing the side effects. From the chemical structures of HIV protease inhibitors and their possible off-target molecules, we could obtain hints for optimizing the molecular selectivity of the inhibitors, to provide help in the design of new compounds with enhanced bioavailability and reduced side effects.

Keywords: glucose transporter-4; off-target; proteasome; side effect.

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Figures

Figure 1
Figure 1
The HIV-1 protease structure in complex with an inhibitor.
Figure 2
Figure 2
Chemical structures of the HIV protease inhibitors.
Figure 3
Figure 3
Potential target molecules of the HIV protease inhibitors.
See this image and copyright information in PMC

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