1. Syntheses and evaluation of new acridone derivatives for selective binding of oncogene c-myc promoter i-motifs in gene transcriptional regulation
- Author
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Mingxue Wang, Xiaoya Li, Guo-Tao Kuang, Yan Zhang, Zhi-Shu Huang, Bing Shu, Jia-Heng Tan, Tian-Miao Ou, Jiaojiao Cao, Shuangshuang Kang, Jun Qiu, Meiling Zhang, and Ding Li
- Subjects
0301 basic medicine ,Dna duplex ,Transcription, Genetic ,Down-Regulation ,Antineoplastic Agents ,Apoptosis ,010402 general chemistry ,01 natural sciences ,Catalysis ,Proto-Oncogene Proteins c-myc ,Structure-Activity Relationship ,03 medical and health sciences ,chemistry.chemical_compound ,Transcription (biology) ,Cell Line, Tumor ,Fluorescence Resonance Energy Transfer ,Materials Chemistry ,Transcriptional regulation ,Humans ,Promoter Regions, Genetic ,Gene ,Cell Proliferation ,Tumor cell apoptosis ,Binding Sites ,Dose-Response Relationship, Drug ,Molecular Structure ,Oncogene ,Metals and Alloys ,General Chemistry ,0104 chemical sciences ,Surfaces, Coatings and Films ,Electronic, Optical and Magnetic Materials ,Gene Expression Regulation, Neoplastic ,Acridone ,030104 developmental biology ,Biochemistry ,chemistry ,Ceramics and Composites ,Drug Screening Assays, Antitumor ,Acridones - Abstract
We synthesized a series of acridone derivatives for specific binding ligands of i-motifs. Subsequent evaluations showed that B19 could selectively bind to and stabilize the c-myc promoter i-motif without significant binding to the G-quadruplex and duplex DNA. This caused down-regulation of c-myc transcription and expression, resulting in tumor cell apoptosis.
- Published
- 2018
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