Monchaud David, Teulade-Fichou Marie-Paule
Institut Curie, Section Recherche, CNRS UMR 176, Center Universitaire Paris XI, Orsay, France.
Methods Mol Biol. 2010;608:257-71. doi: 10.1007/978-1-59745-363-9_15.
Currently, small molecules able to interact specifically with G-quadruplex DNA (G-quadruplex ligands) are intensively studied since they appear to inhibit the growth of cancer cells via an unprecedented mode of action based on structural perturbation of telomeres. It is thus of crucial interest to develop methods that enable easy, rapid and reliable detection of valuable candidates. Herein, we would like to report on the G4-FID assay, a simple fluorescence screening method based on the displacement of a DNA light-up probe (thiazole orange) from both quadruplex and duplex DNA, therefore allowing a concomitant evaluation of the quadruplex-affinity and quadruplex- over duplex-selectivity of the tested candidates.
目前,能够与G-四链体DNA特异性相互作用的小分子(G-四链体配体)正受到深入研究,因为它们似乎通过一种基于端粒结构扰动的前所未有的作用方式来抑制癌细胞的生长。因此,开发能够轻松、快速且可靠地检测有价值候选物的方法至关重要。在此,我们想报道一种G4-FID检测法,这是一种基于DNA发光探针(噻唑橙)从四链体和双链体DNA上被置换的简单荧光筛选方法,因此可以同时评估受试候选物的四链体亲和力和四链体相对于双链体的选择性。