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

doi:10.1039/D3CC00556A

Simple and fast screening for structure-selective G-quadruplex ligands†

Yoshiki Hashimoto,^a Yoshiki Imagawa,^a Kaho Nagano,^a Ryuichi Maeda,^a Naho Nagahama,^a Takeru Torii,^a Natsuki Kinoshita,^a Nagisa Takamiya,^a Keiko Kawauchi,^a Hisae Tatesishi-Karimata,^b Naoki Sugimoto

^ab and Daisuke Miyoshi

*^a

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* Corresponding authors

^a Frontiers of Innovative Research in Science and Technology, Konan university, 7-1-20 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo, Japan

^b Frontier Institute for Biomolecular Engineering Research, Konan university, 7-1-20 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo, Japan

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.

Chemical Communications

Simple and fast screening for structure-selective G-quadruplex ligands†

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Simple and fast screening for structure-selective G-quadruplex ligands

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