Recent advances in the research of HIV-1 RNase H inhibitors

Mini Rev Med Chem. 2008 Oct;8(12):1243-51. doi: 10.2174/138955708786141052.


Reverse transcription is a crucial step in the life cycle of human immunodeficiency virus type 1 (HIV-1). In this process, multiple functional enzymes including RNA-dependent DNA polymerase, DNA-dependent DNA polymerase and RNase H are indispensable. The RNase H functions to degrade RNA of the RNA-DNA heteroduplex into small fragment. These properties of HIV-1 RNase H make it an attractive target for rational anti-HIV-1 drug design and development. In this review, we summarized the HIV-1 RNase H inhibitors that were recently reported in the literature, including their chemical structure, mechanism and structure-activity relationship. It seems likely that HIV-1 RNase H as a prominent non-traditional target may lead to the development of anti-HIV agents which could be used alone or in the combination with other HIV inhibitors in AIDS chemotherapy.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Amino Acid Sequence
  • Anti-HIV Agents / pharmacology*
  • Catalytic Domain
  • Chemistry, Pharmaceutical / methods
  • Drug Design
  • HIV Infections / drug therapy*
  • HIV-1 / enzymology*
  • Humans
  • Ions
  • Models, Chemical
  • Molecular Conformation
  • Molecular Sequence Data
  • Protein Conformation
  • Ribonuclease H / metabolism*
  • Structure-Activity Relationship


  • Anti-HIV Agents
  • Ions
  • Ribonuclease H