Stabilization of G-quadruplex DNA and inhibition of Bcl-2 expression by a pyridostatin analog
Stabilization of G-quadruplex DNA and inhibition of Bcl-2 expression by a pyridostatin analog
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吡啶他汀类似物稳定 G-四链体 DNA 并抑制 Bcl-2 表达
DOI：
10.1016/j.bmcl.2016.02.065
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发表时间：
2016-04-01
影响因子：
2.7
通讯作者：
Tang, Yalin
中科院分区：
文献类型：
--
作者：
Feng, Yun;Yang, Dazhang;Tang, Yalin
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.
