Oligonucleotide conjugate GRN163L targeting human telomerase as potential anticancer and antimetastatic agent

Sergei M. Gryaznov, Shalmica Jackson, Gunnur Dikmen, Calvin Harley, Brittney Shea Herbert, Woodring E. Wright, Jerry W. Shay

Research output: Contribution to journalArticle

22 Citations (Scopus)

Abstract

Telomerase is one of the key enzymes responsible for the proliferative immortality of the majority of cancer cells. We recently introduced a new telomerase inhibitor, a 13-mer oligonucleotide N3′ → P5′-thio-phosphoramidate lipid conjugate, designated as GRN163L. This compound inhibits telomerase activity in various tumor cell lines with IC50 values of 3-300 nM without any cellular uptake enhancers. GRN163L demonstrated potent and sequence specific anti-cancer activity in vivo in multiple animal models. This compound was able to significantly affect not only the growth of primary tumors, but also the spread and proliferation of metastases. GRN163L is currently in Phase I and Phase I/II clinical studies in patients with solid tumors and CLL, respectively.

Original languageEnglish (US)
Pages (from-to)1577-1579
Number of pages3
JournalNucleosides, Nucleotides and Nucleic Acids
Volume26
Issue number10-12
DOIs
StatePublished - Oct 2007

Fingerprint

Telomerase
Oligonucleotides
Antineoplastic Agents
Tumors
Cells
Neoplasms
Animals
Tumor Cell Line
Inhibitory Concentration 50
Lipids
Animal Models
Enzymes
Neoplasm Metastasis
Growth

Keywords

  • Adhesion
  • Anticancer
  • GRN163L
  • Morphology
  • Phosphoramidates
  • Telomerase

ASJC Scopus subject areas

  • Genetics
  • Biochemistry

Cite this

Oligonucleotide conjugate GRN163L targeting human telomerase as potential anticancer and antimetastatic agent. / Gryaznov, Sergei M.; Jackson, Shalmica; Dikmen, Gunnur; Harley, Calvin; Herbert, Brittney Shea; Wright, Woodring E.; Shay, Jerry W.

In: Nucleosides, Nucleotides and Nucleic Acids, Vol. 26, No. 10-12, 10.2007, p. 1577-1579.

Research output: Contribution to journalArticle

Gryaznov, Sergei M. ; Jackson, Shalmica ; Dikmen, Gunnur ; Harley, Calvin ; Herbert, Brittney Shea ; Wright, Woodring E. ; Shay, Jerry W. / Oligonucleotide conjugate GRN163L targeting human telomerase as potential anticancer and antimetastatic agent. In: Nucleosides, Nucleotides and Nucleic Acids. 2007 ; Vol. 26, No. 10-12. pp. 1577-1579.
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