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

6 Citations (Scopus)

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
Externally publishedYes

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Telomerase
Oligonucleotides
Assays
RNA
Enzymes
phosphoramidic acid

Keywords

  • Oligonucleotide thio-phosphoramidates
  • Telomerase inhibitors

ASJC Scopus subject areas

  • Genetics
  • Biochemistry

Cite this

Novel short oligonucleotide conjugates as inhibitors of human telomerase. / Pongracz, Krisztina; Li, Shihong; Herbert, Brittney-Shea; Pruzan, Ronald; Wunder, Ellen; Chin, Allison; Piatyszek, Mieczyslaw; Shay, Jerry; Gryaznov, Sergei M.

In: Nucleosides, Nucleotides and Nucleic Acids, Vol. 22, No. 5-8, 2003, p. 1627-1629.

Research output: Contribution to journalArticle

Pongracz, K, Li, S, Herbert, B-S, Pruzan, R, Wunder, E, Chin, A, Piatyszek, M, Shay, J & Gryaznov, SM 2003, 'Novel short oligonucleotide conjugates as inhibitors of human telomerase', Nucleosides, Nucleotides and Nucleic Acids, vol. 22, no. 5-8, pp. 1627-1629. https://doi.org/10.1081/NCN-120023085
Pongracz, Krisztina ; Li, Shihong ; Herbert, Brittney-Shea ; Pruzan, Ronald ; Wunder, Ellen ; Chin, Allison ; Piatyszek, Mieczyslaw ; Shay, Jerry ; Gryaznov, Sergei M. / Novel short oligonucleotide conjugates as inhibitors of human telomerase. In: Nucleosides, Nucleotides and Nucleic Acids. 2003 ; Vol. 22, No. 5-8. pp. 1627-1629.
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