Novel short oligonucleotide conjugates as inhibitors of human telomerase

Krisztina Pongracz, Shihong Li, Brittney Shea Herbert, Ronald Pruzan, Ellen Wunder, Allison Chin, Mieczyslaw Piatyszek, Jerry Shay, Sergei M. Gryaznov

Research output: Contribution to journalArticle

7 Scopus citations

Abstract

A series of oligonucleotide conjugates were designed and synthesized as novel inhibitors of human telomerase. These compounds contain a relatively short (6-7-mer) oligonucleotide domain, with an N3′ → P5′ phosphoramidate (np) or thio-phosphoramidate (nps) backbone, targeted to the template region of the RNA component of the enzyme and various pendant groups attached to either their 5′- or preferably to the 3′- termini. The most potent compounds in the series inhibited telomerase with low nM IC 50 values in biochemical assays whereas the cognate oligonucleotides without the pendant groups were significantly less active having IC 50 values 100-1000-fold higher.

Original languageEnglish (US)
Pages (from-to)1627-1629
Number of pages3
JournalNucleosides, Nucleotides and Nucleic Acids
Volume22
Issue number5-8
DOIs
StatePublished - 2003

Keywords

  • Oligonucleotide thio-phosphoramidates
  • Telomerase inhibitors

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Genetics

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