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

23 Scopus citations

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 1 2007

Keywords

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

ASJC Scopus subject areas

  • Genetics
  • Biochemistry

Fingerprint Dive into the research topics of 'Oligonucleotide conjugate GRN163L targeting human telomerase as potential anticancer and antimetastatic agent'. Together they form a unique fingerprint.

  • Cite this