[The influence of compound aITEL1296 on telomerase activity and the growth of cancer cells].
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.
N A
NA
Kovalenko
D D
DD
Zhdanov
M V
MV
Bibikova
V Iu
VIu
Gotovtseva
D062365:Aminobenzoates / Q000494:pharmacology; D000903:Antibiotics, Antineoplastic / Q000302:isolation & purification / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects*; D004261:DNA Replication / Q000187:drug effects; D005347:Fibroblasts / Q000166:cytology / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D019169:Jurkat Cells; D009281:Naphthalenes / Q000494:pharmacology; D009369:Neoplasms / Q000201:enzymology* / Q000473:pathology; D018894:Reverse Transcriptase Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D013302:Streptomyces / Q000737:chemistry; D019098:Telomerase / Q000037:antagonists & inhibitors*
D062365:Aminobenzoates; D000903:Antibiotics, Antineoplastic; C458523:BIBR 1532; D009281:Naphthalenes; D018894:Reverse Transcriptase Inhibitors; D019098:Telomerase