The influence of compound itel1296 on telomerase activity and the growth of cancer cells

   
Kovalenko N.A.1, Zhdanov D.D.2 , Bibikova M.V.3, Gotovtseva V.Y.3

1. I.M. Sechenov First Moscow State Medical University, Research Center
2. Institute of Biomedical Chemistry of Russian Academy of Medical Sciences Peoples` Friendship University of Russia, Ecological Faculty
3. National Research Center of Antibiotics
Section: Experimental/Clinical Study
DOI: 10.18097/PBMC20115705501      UDK: 615.014.23.417      PubMed Id: 22629600
Year: 2011  Volume: 57  Issue: 5  Pages: 501-510
Telomerase is a ribonucleoprotein that synthesizes telomeric repeats and identified as a promising target for anticancer therapy. Here we describe a new compound aITEL1296 as a potent telomerase inhibitor. 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. Besides 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.
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Kovalenko N.A., Zhdanov D.D., Bibikova M.V., Gotovtseva V.Y. (2011) Biomeditsinskaya khimiya, 57(5), 501-510.
This paper is also available as the English translation:10.1134/S1990750812010064
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