Aptamers that recognize drug-resistant HIV-1 reverse transcriptase

Nucleic Acids Res. 2008 Dec;36(21):6739-51. doi: 10.1093/nar/gkn775. Epub 2008 Oct 23.

Abstract

Drug-resistant variants of HIV-1 reverse transcriptase (RT) are also known to be resistant to anti-RT RNA aptamers. In order to be able to develop diagnostics and therapies that can focus on otherwise drug-resistant viruses, we have isolated two aptamers against a well-known, drug-resistant HIV-1 RT, Mutant 3 (M3) from the multidrug-resistant HIV-1 RT panel. One aptamer, M302, bound M3 but showed no significant affinity for wild-type (WT) HIV-1 RT, while another aptamer, 12.01, bound to both M3 and WT HIV-1 RTs. In contrast to all previously selected anti-RT aptamers, neither of these aptamers showed observable inhibition of either polymerase or RNase H activities. Aptamers M302 and 12.01 competed with one another for binding to M3, but they did not compete with a pseudoknot aptamer for binding to the template/primer cleft of WT HIV-1 RT. These results represent the surprising identification of an additional RNA-binding epitope on the surface of HIV-1 RT. M3 and WT HIV-1 RTs could be distinguished using an aptamer-based microarray. By probing protein conformation as a correlate to drug resistance we introduce an additional and useful measure for determining HIV-1 drug resistance.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Anti-HIV Agents / therapeutic use
  • Aptamers, Nucleotide / chemistry*
  • Base Sequence
  • Drug Resistance, Viral / genetics*
  • HIV Reverse Transcriptase / analysis*
  • HIV Reverse Transcriptase / chemistry
  • HIV Reverse Transcriptase / genetics
  • HIV-1 / drug effects*
  • HIV-1 / genetics
  • Molecular Sequence Data
  • Mutation
  • Nucleic Acid Conformation
  • Protein Array Analysis

Substances

  • Anti-HIV Agents
  • Aptamers, Nucleotide
  • reverse transcriptase, Human immunodeficiency virus 1
  • HIV Reverse Transcriptase