Simple and fast screening for structure-selective G-quadruplex ligands
Yoshiki Hashimoto, Yoshiki Imagawa, Kaho Nagano, Ryuichi Maeda, Naho Nagahama, Takeru Torii, Natsuki Kinoshita, Nagisa Takamiya, Keiko Kawauchi, Hisae Tatesishi-Karimata, Naoki Sugimoto, Daisuke Miyoshi
Abstract
Structural selectivity of G-quadruplex ligands is essential for cellular applications since there is an excess of nucleic acids forming duplex structures compared to G-quadruplex structures in living cells. In this study, we developed new structure-selective G-quadruplex ligands utilizing a simple and fast screening system. The affinity, selectivity, enzymatic inhibitory activity and cytotoxicity of the structure-selective G-quadruplex ligands were demonstrated along with a structural selectivity-cytotoxicity relationship of G-quadruplex ligands.