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题名: Stabilization of G-quadruplex DNA and inhibition of Bcl-2 expression by a pyridostatin analog
作者: Feng, Yun1; Yang, Dazhang1; Chen, Hongbo2; Cheng, Wenli3; Wang, Lixia2; Sun, Hongxia2; Tang, Yalin2
关键词: Bcl-2 gene ; P1 promoter ; G-quadruplex ; Pyridostatin analog ; Transcription
刊名: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
发表日期: 2016-04-01
卷: 26, 期:7, 页:1660-1663
收录类别: SCI
英文摘要: The G-quadruplexes located in the P1 promoter of B-cell lymphoma-2 (Bcl-2) gene are implicated to regulate Bcl-2 expression. Here, we designed a new pyridostatin analog named PDF, which exhibited high specificity and stabilizing effect toward G-quadruplexes. The luciferase assay demonstrated that PDF could significantly suppress Bcl-2 transcriptional activation in human laryngeal squamous carcinoma cells (Hep-2) cells. Besides, PDF also induced cell apoptosis in vitro assays. These results provide an excellent G-quadruplex specific ligand as an efficient Bcl-2 inhibitor. These results also implicate that PDF may be a potential anticancer drug to head neck cancer. (C) 2016 Elsevier Ltd. All rights reserved.
语种: 英语
内容类型: 期刊论文
URI标识: http://ir.iccas.ac.cn/handle/121111/35882
Appears in Collections:分子动态与稳态结构实验室_期刊论文

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作者单位: 1.China Japan Friendship Hosp, Dept Otolaryngol, Beijing 100029, Peoples R China
2.Chinese Acad Sci, Beijing Natl Lab Mol Sci, State Key Lab Struct Chem Unstable & Stable Speci, Inst Chem, Beijing 100190, Peoples R China
3.China Japan Friendship Hosp, Dept Cardiol, Beijing 100029, Peoples R China
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