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

ABSTRACT: 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.

SUBMITTER: Xiong YX

PROVIDER: S-EPMC5600358 | biostudies-literature | 2016 Mar

REPOSITORIES: biostudies-literature

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

Xiong Yun-Xia YX Chen Ai-Chun AC Yao Pei-Fen PF Zeng De-Ying DY Lu Yu-Jing YJ Tan Jia-Heng JH Huang Zhi-Shu ZS Ou Tian-Miao TM

Biochemistry and biophysics reports 20160114

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. ...[more]

PMID: 28955841

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