Structural biology of HIV-1 reverse transcriptase allosteric inhibitors for drug design
Zhenzhen Zhou, Yanying Sun, Da Feng, Zhao Wang, Fabao Zhao, Shenghua Gao, Peng Zhan, Dongwei Kang, Xinyong Liu
TL;DR
This paper reviews the structural biology of HIV-1 reverse transcriptase inhibitors to guide the design of more effective anti-HIV drugs.
Contribution
A comprehensive review of recent co-crystal structures of allosteric inhibitors with HIV-1 RT for drug development.
Findings
Co-crystal structures of small molecule inhibitors with HIV-1 RT have advanced drug design.
Allosteric inhibitors show high efficiency and low toxicity, making them promising drug candidates.
Structural insights help identify strategies for developing next-generation anti-HIV drugs.
Abstract
HIV-1 reverse transcriptase (RT) is responsible for reverse transcription of viral single-stranded RNA to double-stranded DNA, which plays an important role in the replication cycle of HIV-1 and has been identified as a key target for anti-HIV-1 drug discovery. Among HIV-1 RT inhibitors, allosteric inhibitors acting on non-catalytic sites have the advantages of high efficiency and low cytotoxicity, which are the focus of the research on anti-HIV-1 inhibitors. Great progress has been achieved in the structural biology of HIV-1 RT, which significantly facilitated the development of RT allosteric inhibitors. Herein, we provided a detailed review of the co-crystal structures of small molecule allosteric inhibitors in complex with RT reported in the last decade. Moreover, the strategies to discover novel and efficient inhibitors based on co-crystal structures have also been discussed,…
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Taxonomy
TopicsHIV/AIDS drug development and treatment · HIV Research and Treatment · Crystallography and molecular interactions