Oligonucleotide inhibitors of HIV-1 integrase efficiently inhibit HIV-1 reverse transcriptase

S. P. Korolev, T. S. Zatsepin, M. B. Gottikh

Research output: Contribution to journalArticlepeer-review

Abstract

The impact of conjugates of 11-mer 2′-О-methyl oligoribonucleotides with eosin and 6-carboxy-4,7,2′,4′,5′,7′-hexachlorofluorescein on the functioning of HIV-1 reverse transcriptase (RT) was studied. These compounds were shown to inhibit the activity of RT RNase H domain. The inhibition efficiency was higher for eosin conjugates and did not depend on the oligonucleotide primary structure. The eosin conjugates were also found to block the RT polymerase activity including the mutant proteins resistant to nonnucleoside inhibitors. Since the conjugates are efficient inhibitors of HIV-1 integrase, we can assume that they belong to a new class of HIV-1 dual acting inhibitors, potentially capable of blocking several initial stages of the viral replication cycle.

Original languageEnglish
Pages (from-to)135-139
Number of pages5
JournalRussian Journal of Bioorganic Chemistry
Volume43
Issue number2
DOIs
Publication statusPublished - 1 Mar 2017
Externally publishedYes

Keywords

  • HIV-1
  • oligonucleotide inhibitors
  • reverse transcriptase
  • RNase H

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