HIV protease inhibitors: a review of molecular selectivity and toxicity

Abstract

Zhengtong Lv,* Yuan Chu,* Yong Wang Department of Immunology, School of Basic Medical Science, Xiangya School of Medicine, Central South University, Changsha, Hunan, People's Republic of China *Both authors contributed equally to this work 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: off-target, side effect, glucose transporter-4, proteasome