A Competitive Pull-Down Assay Using G-quadruplex DNA Linked Magnetic Nanoparticles To Determine Specificity of G-quadruplex Ligands

被引:32
作者
Panda, Deepanjan [1 ]
Saha, Puja [1 ]
Chaudhuri, Ritapa [1 ]
Prasanth, Thumpati [1 ,2 ]
Ravichandiran, Velayutham [2 ]
Dash, Jyotirmayee [1 ]
机构
[1] Indian Assoc Cultivat Sci, Sch Chem Sci, Kolkata 700032, India
[2] Natl Inst Pharmaceut Educ & Res, Kolkata 700032, India
关键词
C-MYC; SMALL-MOLECULE; PROMOTER; BINDING; MITOXANTRONE; TARGET; BCL-2; PROBE; SITE;
D O I
10.1021/acs.analchem.9b00889
中图分类号
O65 [分析化学];
学科分类号
070302 ; 081704 ;
摘要
Herein, we develop a competitive screening method in which G-quadruplex DNA linked magnetic nanoparticles pull down selective ligands for a particular quadruplex topology from a series of small molecules. The screening strategy is first optimized with known G-quadruplex ligands and then used with a new series of G-quadruplex interactive bis-triazolyl ligands that are synthesized by Cu(I)-catalyzed azide alkyne cycloaddition. The assay enables the identification of c-MYC and BCL2 G-quadruplex selective bis-triazole ligands that specifically target promoter G-quadruplexes in cancer cells.
引用
收藏
页码:7705 / 7711
页数:7
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