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

초록

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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