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Current Medicinal Chemistry
ISSN (Print): 0929-8673
ISSN (Online): 1875-533X
DOI: 10.2174/0929867321666140120121158      Price:  $58

Recent Progress in the Research of Small Molecule HIV-1 RNase H Inhibitors

Author(s): Lili Cao, Weiguo Song, Erik De Clercq, Peng Zhan and Xinyong Liu
Pages 1956-1967 (12)
Reverse transcription of human immunodeficiency virus type 1 (HIV-1) is a crucial step in the life cycle initiated by the viral-coded reverse transcriptase (RT), functioning as RNA- and DNA-dependent DNA polymerase (RDDP and DDDP) and the ribonuclease H (RNase H). The RNase H functions to degrade the RNA strand of the RNA:DNA heteroduplex, which makes it an attractive target for rational anti-HIV-1 drug design and development. Although development of drugs targeting the DNA polymerase have been highly successful, the discovery of drugable inhibitors of HIV RNase H is still in its infancy and none of RNase H inhibitors has reached the clinical development stage currently. This review describes the recent progress in the HIV-1 RNase H inhibitors, focusing on their chemical feature, mechanism and the structure-activity relationship (SAR).
AIDS, drug design, HIV-1, RNase H inhibitors, RT, SAR.
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, 250012, Jinan, Shandong, P.R.China.