Drug name: Imetelstat


Related CSCTT Targets

TERT [ref.1]O14746

Imetelstat

Cas.no PubChem ID
868169-64-6 71587831
Known Target
TERTO14746
Introduction
Imetelstat a synthetic lipid-conjugated, 13-mer oligonucleotide N3' P5'-thio-phosphoramidate with potential antineoplastic activity. Complementary to the template region of telomerase RNA (hTR), imetelstat acts as a competitive enzyme inhibitor that binds and blocks the active site of the enzyme (a telomerase template antagonist), a mechanism of action which differs from that for the antisense oligonucleotide-mediated inhibition of telomerase activity through telomerase mRNA binding. Inhibition of telomerase activity in tumor cells by imetelstat results in telomere shortening, which leads to cell cycle arrest or apoptosis.

Imetelstat-Structure

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Reference

  • [1] Neural tumor-initiating cells have distinct telomere maintenance and can be safely targeted for telomerase inhibition.
    Castelo-Branco, P., et al. (2011). Clin Cancer Res 17(1): 111-121. [ 21208905 ]

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