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.