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Telomerase is a ribonucleoprotein complex, which synthesizes telomeric repeats and which has been identified as a promising target for anticancer therapy. Here we have investigated the effect of a new compound aITEL1296 on telomerase activity. aITEL1296 effectively inhibited telomerase activity; its inhibitory activity was a bit higher (IC50 = 0.19 ± 0.02 ng/mL) than that of BIBR1532, one of the most potent telomerase inhibitors known to date. In addition to telomerase inhibition aITEL1296 activated apoptotic mechanisms and effectively suppressed proliferation of tumor cell lines (GI50 = 5.0 ± 0.2 ng/mL for most sensitive cell line LnCap) but not normal fibroblast cell line.

Authors:   N. A. Kovalenko, D. D. Zhdanov, M. V. Bibikova, V. Y. Gotovtseva
Journal:   Biochemistry Supplemental Series B: Biomedical Chemistry
Year:   2012
DOI:   10.1134/S1990750812010064
Publication date:   06-03-2012

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