Telomerase as a potential molecular target to study G-quartet phosphorothioates

Antisense Nucleic Acid Drug Dev. 1996 Spring;6(1):3-7. doi: 10.1089/oli.1.1996.6.3.

Abstract

Inhibition of gene expression by phosphorothioate oligomers is complex and involves specific and nonspecific mechanisms. Oligomers that contain a G-quartet elicit distinct effects in vitro and in vivo that are dependent on the context of the G-quartet's occurrence within a sequence. The enzyme telomerase, a ribonucleoprotein, has a stretch of C residues in the RNA template, which are used to add terminal dG-rich telomeric repeats to the ends of chromosomes. Some but not all phosphorothioates containing a G-quartet, depending on the context of occurrence, inhibited telomerase activity in vitro. Non-G-quartet phosphorothioates did not inhibit this activity. Activities of control enzymes, such as reverse transcriptase or taq polymerase, were not affected by the G-quartet oligomers. Neither phosphodiester nor chimeric oligomers of a G-quartet-containing oligomer were as potent inhibition of telomerase activity as phosphorothioate oligomers. These results may provide a molecular target to study the effects of G-quartet-containing oligomers.

MeSH terms

  • Animals
  • Base Sequence
  • Cell Line
  • DNA Primers
  • Fibrosarcoma
  • Guanine
  • Mice
  • NF-kappa B / genetics
  • Oligonucleotides, Antisense / chemistry*
  • Oligonucleotides, Antisense / metabolism
  • Polymerase Chain Reaction
  • Structure-Activity Relationship
  • Telomerase / metabolism*
  • Thionucleotides*
  • Transcription Factor RelA
  • Tumor Cells, Cultured

Substances

  • DNA Primers
  • NF-kappa B
  • Oligonucleotides, Antisense
  • Thionucleotides
  • Transcription Factor RelA
  • Guanine
  • Telomerase