A transcription factor hijacking to regulate RAR alpha by using a chimeric molecule of retinoic acid and a DNA alkylator

作者：Min Kyung Hoon; Yun Byoung Gu; Lee Yoonsung; Song Jiho; Ham Won Hoon; Lee YoungJoo; Park Hyun Ju^*

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(14): 4248-4251.

DOI：10.1016/j.bmcl.2011.05.062

• Transcription factor hijacking
• Chimeric molecule
• Chlorambucil
• All-trans retinoic acid
• Retinoic acid receptor alpha

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.

• 出版日期2011-7-15