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