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

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.

Automated summary

In this study, new structure-selective G-quadruplex ligands were developed using a simple and fast screening system. The affinity, selectivity, enzymatic inhibitory activity and cytotoxicity of these ligands were demonstrated, along with a relationship between their structural selectivity and cytotoxicity.