Properties of quadruplex oligonucleotides with anti-HIV-1 activity

Nucleic Acids Symp Ser. 2000;(44):181-2. doi: 10.1093/nass/44.1.181.


A phosphorothioate oligonucleotide composed of deoxyguanosine and thymidine was identified as an inhibitor of HIV-1 infection at an early stage of the HIV-1 replication cycle in vitro. The phosphodiester and phosphorothioate chimeric oligonucleotides were found to be potent inhibitors of several steps of HIV-1 infection: the interaction with CD4 and the chemokine receptor, the reverse transcriptase activity, and the integrase activity. To elucidate the mechanism of the anti-HIV-1 function of these oligonucleotides in terms of their structure, we focussed on their G-serial sequences and investigated the characteristics of their solution structures. These oligonucleotides were proved to be able to adopt G-quadruplex structures by UV and CD measurements. We presume that the anti-HIV-1 activities of these oligonucleotides are consequently attributable to G-quadruplex formation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemistry*
  • Anti-HIV Agents / pharmacology*
  • Base Sequence
  • HIV-1 / drug effects*
  • HIV-1 / physiology
  • Humans
  • In Vitro Techniques
  • Nucleic Acid Conformation
  • Oligodeoxyribonucleotides / chemistry*
  • Oligodeoxyribonucleotides / pharmacology*
  • Spectrophotometry
  • Thionucleotides / chemistry
  • Thionucleotides / pharmacology
  • Virus Replication / drug effects


  • Anti-HIV Agents
  • Oligodeoxyribonucleotides
  • Thionucleotides