The HIV-1 reverse transcription (RT) process as target for RT inhibitors

Med Res Rev. 2000 Mar;20(2):129-54. doi: 10.1002/(sici)1098-1128(200003)20:2<129::aid-med2>;2-a.


Since the Human Immunodeficiency Virus Type 1 (HIV-1) was identified as the etiologic agent of the Acquired Immune Deficiency Syndrome (AIDS), the HIV-1 reverse transcriptase (RT) has been the subject of intensive study. The reverse transcription entails the transition of the single-stranded viral RNA into double-stranded proviral DNA, which is then integrated into the host chromosome. Therefore, the HIV-1 reverse transcriptase plays a pivotal role in the life cycle of the virus and is consequently an interesting target for anti-HIV drug therapy. In the first section, we describe the complex process of reverse transcription and the different activities involved in this process. We then highlight the structure-function relationship of the HIV-1 reverse transcriptase, which is of great importance for a better understanding of resistance development, a major problem in anti-AIDS therapies. Finally, we summarize the mechanisms of HIV resistance toward various RT inhibitors and the implications thereof for the current anti-HIV drug therapies.

Publication types

  • Review

MeSH terms

  • Anti-HIV Agents / pharmacology
  • Drug Resistance, Microbial / genetics
  • HIV Reverse Transcriptase / chemistry
  • HIV Reverse Transcriptase / genetics
  • HIV Reverse Transcriptase / metabolism*
  • HIV-1 / drug effects
  • HIV-1 / genetics
  • Protein Conformation
  • Reverse Transcriptase Inhibitors / pharmacology
  • Structure-Activity Relationship
  • Transcription, Genetic*


  • Anti-HIV Agents
  • Reverse Transcriptase Inhibitors
  • HIV Reverse Transcriptase