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).
Keywords: AIDS, drug design, HIV-1, RNase H inhibitors, RT, SAR.
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