Telomerase inhibitors - Oligonucleotide phosphoramidates as potential therapeutic agents

S. Gryaznov, K. Pongracz, T. Matray, R. Schultz, R. Pruzan, J. Aimi, A. Chin, C. Harley, Brittney-Shea Herbert, J. Shay, Y. Oshima, A. Asai, Y. Yamashita

Research output: Contribution to journalArticle

57 Citations (Scopus)

Abstract

We have designed, synthesized, and evaluated using physical, chemical and biochemical assays various oligonucleotide N3′ → P5′ phosphoramidates, as potential telomerase inhibitors. Among the prepared compounds were 2′-deoxy, 2′-hydroxy, 2′-methoxy, 2′-ribo-fluoro, and 2′-arabino-fluoro oligonucleotide phosphoramidates, as well as novel N3′ → P5′ thio-phosphoramidates. The compounds demonstrated sequence specific and dose dependent activity with IC50 values in the sub-nM to pM concentration range.

Original languageEnglish (US)
Pages (from-to)401-410
Number of pages10
JournalNucleosides, Nucleotides and Nucleic Acids
Volume20
Issue number4-7
DOIs
StatePublished - 2001
Externally publishedYes

Fingerprint

Telomerase
Oligonucleotides
Inhibitory Concentration 50
Assays
Therapeutics
phosphoramidic acid

ASJC Scopus subject areas

  • Genetics
  • Biochemistry

Cite this

Gryaznov, S., Pongracz, K., Matray, T., Schultz, R., Pruzan, R., Aimi, J., ... Yamashita, Y. (2001). Telomerase inhibitors - Oligonucleotide phosphoramidates as potential therapeutic agents. Nucleosides, Nucleotides and Nucleic Acids, 20(4-7), 401-410. https://doi.org/10.1081/NCN-100002314

Telomerase inhibitors - Oligonucleotide phosphoramidates as potential therapeutic agents. / Gryaznov, S.; Pongracz, K.; Matray, T.; Schultz, R.; Pruzan, R.; Aimi, J.; Chin, A.; Harley, C.; Herbert, Brittney-Shea; Shay, J.; Oshima, Y.; Asai, A.; Yamashita, Y.

In: Nucleosides, Nucleotides and Nucleic Acids, Vol. 20, No. 4-7, 2001, p. 401-410.

Research output: Contribution to journalArticle

Gryaznov, S, Pongracz, K, Matray, T, Schultz, R, Pruzan, R, Aimi, J, Chin, A, Harley, C, Herbert, B-S, Shay, J, Oshima, Y, Asai, A & Yamashita, Y 2001, 'Telomerase inhibitors - Oligonucleotide phosphoramidates as potential therapeutic agents', Nucleosides, Nucleotides and Nucleic Acids, vol. 20, no. 4-7, pp. 401-410. https://doi.org/10.1081/NCN-100002314
Gryaznov, S. ; Pongracz, K. ; Matray, T. ; Schultz, R. ; Pruzan, R. ; Aimi, J. ; Chin, A. ; Harley, C. ; Herbert, Brittney-Shea ; Shay, J. ; Oshima, Y. ; Asai, A. ; Yamashita, Y. / Telomerase inhibitors - Oligonucleotide phosphoramidates as potential therapeutic agents. In: Nucleosides, Nucleotides and Nucleic Acids. 2001 ; Vol. 20, No. 4-7. pp. 401-410.
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