Discovery of novel anti-HIV active G-quadruplex-forming oligonucleotides

Chem Commun (Camb). 2011 Feb 28;47(8):2363-5. doi: 10.1039/c0cc04751a. Epub 2010 Dec 16.

Abstract

A series of d((5')TGGGAG(3')) sequences, 5'-conjugated with a variety of aromatic groups through phosphodiester linkages, were synthesized, showing CD spectra diagnostic of parallel-stranded, tetramolecular G-quadruplex structures. When tested for anti-HIV-1 and HIV-2 activity, potent inhibition of HIV-1 infection in CEM cell cultures was found, associated with high selectivity index values. Surface Plasmon Resonance assays revealed specific binding to HIV-1 gp120 and gp41.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / chemistry*
  • Anti-HIV Agents / pharmacology
  • Cell Line
  • Drug Evaluation, Preclinical
  • G-Quadruplexes*
  • HIV / metabolism
  • HIV Envelope Protein gp120 / chemistry
  • HIV Envelope Protein gp120 / metabolism
  • HIV Envelope Protein gp41 / chemistry
  • HIV Envelope Protein gp41 / metabolism
  • Humans
  • Oligonucleotides / chemical synthesis
  • Oligonucleotides / chemistry*
  • Oligonucleotides / pharmacology
  • Surface Plasmon Resonance

Substances

  • Anti-HIV Agents
  • HIV Envelope Protein gp120
  • HIV Envelope Protein gp41
  • Oligonucleotides