Proceedings of the PSK Conference (대한약학회:학술대회논문집)
- 2003.10b
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- Pages.180.1-180.1
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- 2003
Synthesis of New 3-Arylisoquinolinamines: Effect on Topoisomerase I Inhibition and Cytotoxicity
- Cho, Won-Jae (College of Pharmacy, Chonnam National University) ;
- Min, Sun-Young (College of Pharmacy, Chonnam National University) ;
- Le, Thanh-Nguyen (College of Pharmacy, Chonnam National University) ;
- Kim, Tae-Sung (College of Pharmacy, Chonnam National University)
- Published : 2003.10.01
Abstract
Eukaryotic DNA topoisomerase I (top I) is an essential enzyme that act to relax supercoiled DNA during the transcription, replication and mitosis. Intracellular levels of top I are elevated in a number of human solid tumors, relative to the respective normal tissues, suggesting that controlling the topI level is important to treat cancer. Top I poisons show their antitumor activities by stabilizing the cleavable ternary complex consisting of top I enzyme, DNA, and drug. Thus, top I is a promising target for the development of new cancer chemotherapeutics against a number of solid tumors. (omitted)
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