Blocking the binding of WT1 to bcl-2 promoter by G-quadruplex ligand SYUIQ-FM05

Autor: Yun-Xia Xiong, Ai-Chun Chen, Pei-Fen Yao, De-Ying Zeng, Yu-Jing Lu, Jia-Heng Tan, Zhi-Shu Huang, Tian-Miao Ou
Jazyk: angličtina
Rok vydání: 2016
Předmět:
Zdroj: Biochemistry and Biophysics Reports, Vol 5, Iss C, Pp 346-352 (2016)
Druh dokumentu: article
ISSN: 2405-5808
DOI: 10.1016/j.bbrep.2015.12.014
Popis: At present, wt1, a Wilms’ tumor suppressor gene, is recognized as a critical regulator of tumorigenesis and a potential therapeutic target. WT1 shows the ability to regulate the transcription of bcl-2 by binding to a GC-rich region in the promoter, which can then fold into a special DNA secondary structure called the G-quadruplex. This function merits the exploration of the effect of a G-quadruplex ligand on the binding and subsequent regulation of WT1 on the bcl-2 promoter. In the present study, WT1 was found to bind to the double strand containing the G-quadruplex-forming sequence of the bcl-2 promoter. However, the G-quadruplex ligand SYUIQ-FM05 effectively blocked this binding by interacting with the GC-rich sequence. Our new findings are significant in the exploration of new strategies to block WT1's transcriptional regulation for cancer-cell treatment.
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