title: A transcription factor hijacking to regulate RARα by using a chimeric molecule of retinoic acid and a DNA alkylator.
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 α (RARα) and DNA. The interaction between RA-mustard with RARα was confirmed by binding assay using RARα-overexpressing cell extract. RA-mustard-modified DNA diminished the RARα-dependent luciferase expression in the RARα-abundant cells.
authors.affiliation: College of Pharmacy, Chung-Ang University, Seoul 156-756, Republic of Korea.
authors.forename: Kyung Hoon
authors.initials: KH
authors.lastname: Min
authors.forename: Byoung-Gu
authors.initials: BG
authors.lastname: Yun
authors.forename: Yoonsung
authors.initials: Y
authors.lastname: Lee
authors.forename: Jiho
authors.initials: J
authors.lastname: Song
authors.forename: Won-Hoon
authors.initials: WH
authors.lastname: Ham
authors.forename: Youngjoo
authors.initials: Y
authors.lastname: Lee
authors.forename: Hyun-Ju
authors.initials: HJ
authors.lastname: Park
mesh_terms: D000477:Alkylating Agents / Q000737:chemistry*; D000818:Animals; D019556:COS Cells; D002699:Chlorambucil / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002522:Chlorocebus aethiops; D003198:Computer Simulation; D004247:DNA / Q000737:chemistry*; D018168:Receptors, Retinoic Acid / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000072482:Retinoic Acid Receptor alpha; D014157:Transcription Factors / Q000378:metabolism*; D014212:Tretinoin / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000477:Alkylating Agents; D018168:Receptors, Retinoic Acid; D000072482:Retinoic Acid Receptor alpha; D014157:Transcription Factors; D002699:Chlorambucil; D014212:Tretinoin; D004247:DNA