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

Abstract

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.

• Authors: H Jonckheere, J Anné, E De Clercq
• Journal: Medicinal research reviews (Med Res Rev) Vol. 20 Issue 2 Pg. 129-54 (Mar 2000) ISSN: 0198-6325 [Print] United States
• PMID: 10723025 (Publication Type: Journal Article, Review)
• Copyright: Copyright 2000 John Wiley & Sons, Inc.

Chemical References

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

Topics

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