Proceedings of the PSK Conference (대한약학회:학술대회논문집)
- 2003.10b
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- Pages.176.2-176.2
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- 2003
Studies on Biochemical Mechanism of DNA Alkylating Agents Tethered to Ligands for Retinoic acid Receptor
- Yun, Byoung-Gu (College of Phamacy, Sungkyunkwan University) ;
- Pyun, Sung-Jae (Department of Bioscience & Biotechnology, Sejong University) ;
- Ji, Sang-Mi (Department of Bioscience & Biotechnology, Sejong University) ;
- Ham, Won-Hoon (Department of Bioscience & Biotechnology, Sejong University) ;
- Lee, Young-Joo (Department of Bioscience & Biotechnology, Sejong University) ;
- Park, Hyun-Ju (Department of Bioscience & Biotechnology, Sejong University)
- Published : 2003.10.01
Abstract
Transcription factors (TF) can bind tightly to specific DNA lesions formed by some anticancer agents. The formation these TF:(drug-modified DNA) complex may disrupt expression of genes critical for cell survival, and it was proved to be one of biochemical mechanisms of anticancer activity. Based on this model, we have designed programmable DNA Alkylating agents that can also attract TF, especially nuclear receptors. As a model compound, we designed drug molecules, RA-mustard and Am580-mustard, that enable to bind both retinoic acid receptor (RAR) and DNA by using molecular modeling techniques, and synthesized them by connecting chlorambucil and ligand for RAR with a linker unit. (omitted)
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