Characterization and antitumor activity of triethylene tetramine, a novel telomerase inhibitor.
Triethylene tetramine (TETA) is a novel ligand for G-quadruplex and has been reported to have many kinds of biological activities, including telomerase inhibition, inducing the senescence of tumor cells, etc. In this study, tumor inhibiting activity of TETA and its mechanism were investigated in HeLa cells, MCF-7 cells and mice transplanted with S180 tumor. Results indicated that TETA inhibited telomerase activity involved in decreasing the expression of human telomerase reverse transcriptase (hTERT). We also observed that a low concentration of TETA had limited ability to inhibit the growth of tumor cells in short-term culture, but it could significantly enhance antitumor activity of traditional antitumor drugs in vitro and in vivo.
Liu
Jianhui
J
Guo
Lixia
L
Yin
Fei
F
Zheng
Xuxu
X
Chen
Gang
G
Wang
Yun
Y
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000494:pharmacology*; D018906:Antineoplastic Agents, Alkylating / Q000627:therapeutic use; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology; D015153:Blotting, Western; D016190:Carboplatin / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003520:Cyclophosphamide / Q000627:therapeutic use; D004317:Doxorubicin / Q000494:pharmacology; D005260:Female; D006367:HeLa Cells; D006801:Humans; D007202:Indicators and Reagents; D051379:Mice; D017239:Paclitaxel / Q000494:pharmacology; D020133:Reverse Transcriptase Polymerase Chain Reaction; D012510:Sarcoma 180 / Q000188:drug therapy; D019098:Telomerase / Q000037:antagonists & inhibitors*; D013778:Tetrazolium Salts; D013844:Thiazoles; D014266:Trientine / Q000494:pharmacology*
D000903:Antibiotics, Antineoplastic; D000970:Antineoplastic Agents; D018906:Antineoplastic Agents, Alkylating; D000972:Antineoplastic Agents, Phytogenic; D007202:Indicators and Reagents; D013778:Tetrazolium Salts; D013844:Thiazoles; D004317:Doxorubicin; D003520:Cyclophosphamide; D016190:Carboplatin; D019098:Telomerase; C022616:thiazolyl blue; D017239:Paclitaxel; D014266:Trientine