Progress on HIV-1 RT inhibitors with novel mechanism of action
10.16438/j.0513-4870.2017-1153
- VernacularTitle:具有新作用机制的HIV-1逆转录酶抑制剂研究进展
- Author:
Zhong-xia ZHOU
1
;
Lin SUN
1
;
Dong-wei KANG
1
;
Zi-hui CHEN
1
;
Miao-miao TANG
1
;
Si-yu LI
1
;
Peng ZHAN
1
;
Xin-yong LIU
1
Author Information
1. Department of Medicinal Chemistry, Key Laboratory of Chemical Biology(Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Ji'nan 250012, China
- Publication Type:REVIEWS
- Keywords:
AIDS;
drug target;
HIV-1;
reverse transcriptase;
inhibitor;
drug design
- From:
Acta Pharmaceutica Sinica
2018;53(5):691-700
- CountryChina
- Language:Chinese
-
Abstract:
HIV-1 reverse transcriptase (RT) plays an important role in HIV-1 life cycle. At present, the listed NRTIs and NNRTIs targeting the RT showed high efficiency as clinical first-line drugs. However, the rapid emergence of multidrug-resistant viruses and significant cumulative drug toxicities compromises antiretroviral therapy efficacy and limits therapeutic options. Therefore, there is an urgent demand for new types of RT inhibitors with novel mechanism of action to address this challenge. In recent years, additional inhibitors with novel mechanism of action have been reported, including nucleic acid competitive inhibitors, reverse transcriptase-directed mutagenesis inhibitors, primers/templates-competitive reverse transcriptase inhibitors, polymerase-RNase H inhibitors, reverse transcription initiation process inhibitors, peptide inhibitors etc., which have brought new hope to the development of novel anti-HIV drugs. This article focuses on the development of these inhibitors.
