Department of Chemical Engineering, National Institute of Technology, Nara college, Yata 22, Yamato-koriyama, Nara 639-1080, Japan.
Soft Matter. 2019 Jun 5;15(22):4454-4459. doi: 10.1039/c9sm00411d.
Designing ligands that selectively target G-quadruplex DNAs has gained attention due to their possible roles in regulation of gene expression and as anti-cancer agents. In this article, we report irradiation-induced ligand binding to G-quadruplex DNAs which offers a novel approach to targeting specific G-quadruplexes. Photoinduced binding to G-quadruplex DNAs was observed for copolymers of poly(vinyl alcohol) carrying a malachite green moiety (PVAMG). This molecule has an aromatic ring with cationic charge, which after irradiation becomes a binding site for G-quadruplex DNA. PVAMGs acted as neutral polymers with no binding affinity under dark conditions. The photoinduced binding was revealed by fluorescence spectroscopy, NMR spectroscopy, UV melting curve, and DNA polymerase stop assay. PVAMGs showed preference to parallel G-quadruplex structures over mixed parallel/antiparallel structures. PVAMGs were found to be noncytotoxic under both dark and irradiated conditions up to a concentration of 20 μM.
由于其在基因表达调控和作为抗癌剂方面的可能作用，设计选择性靶向 G-四链体 DNA 的配体引起了关注。在本文中，我们报告了辐照诱导的配体与 G-四链体 DNA 的结合，这为靶向特定 G-四链体提供了一种新方法。聚（聚乙烯醇）携带的孔雀石绿部分（PVAMG）的共聚物观察到光诱导与 G-四链体 DNA 的结合。该分子具有带有正电荷的芳环，辐照后成为 G-四链体 DNA 的结合位点。在黑暗条件下，PVAMG 作为中性聚合物，没有结合亲和力。光诱导结合通过荧光光谱、NMR 光谱、UV 熔解曲线和 DNA 聚合酶停止测定来揭示。PVAMG 表现出对平行 G-四链体结构的偏好，而不是混合平行/反平行结构。在黑暗和辐照条件下，PVAMG 直到 20 μM 的浓度都没有细胞毒性。
