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
Abstract: 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.
Reference: Kovalenko N.A., Zhdanov D.D., Bibikova M.V., Gotovtseva V.Y., The influence of compound itel1296 on telomerase activity and the growth of cancer cells, Biomeditsinskaya khimiya, 2011, vol:
7. Zhdanov D.D., Kovalenko N.A., Abakumova O.Y., Bibikova M.V,. Gotovtseva V. Y. (2010) 5th International Conference "Genomics, Proteomics, Bioinformatics and Nanobiotechnology for Medicine" Abstract Book, 70. Scholar google search
8. Kim N.W., Piatyszek M.A., Prowse K.R., Harley C.B., West M.D., Ho P.L., Coviello G.M., Wright W.E., Weinrich S.L., Shay J.W. (1994) Science, 266, 2011-2015. CrossRef Scholar google search