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A transcription factor hijacking to regulate RAR alpha by using a chimeric molecule of retinoic acid and a DNA alkylator
- Authors
- Min, Kyung Hoon; Yun, Byoung-Gu; Lee, Yoonsung; Song, Jiho; Ham, Won-Hoon; Lee, YoungJoo; Park, Hyun-Ju
- Issue Date
- Jul-2011
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Transcription factor hijacking; Chimeric molecule; Chlorambucil; All-trans retinoic acid; Retinoic acid receptor alpha
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.21, no.14, pp 4248 - 4251
- Pages
- 4
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 21
- Number
- 14
- Start Page
- 4248
- End Page
- 4251
- ISSN
- 0960-894X
1464-3405
- Abstract
- As a model compound for the transcription factor hijacking mechanism of action of DNA damaging agent that simultaneously bind to the nuclear receptor, we designed and synthesized a chimeric molecule, RA-mustard, which can bind with both retinoic acid receptor alpha (RAR alpha) and DNA. The interaction between RA-mustard with RAR alpha was confirmed by binding assay using RAR alpha-overexpressing cell extract. RA-mustard-modified DNA diminished the RAR alpha-dependent luciferase expression in the RAR alpha-abundant cells. (C) 2011 Elsevier Ltd. All rights reserved.
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