Structure of G-Quadruplex in the Oncogene c-myc Promoter and Small Ligands Targeting the G-Quadruplex

The revealing of the relationship between the G-quadruplex and cancer by modern molecular biology techniques provides a new opportunity to the anti-cancer drugs research. Because of the important effect on cellular proliferation and apoptosis, the G-quadruplex in the c-myc promoter has emerged as an attractive target for anti-cancer therapeutic agents. The present article aims to highlight recent advances in the structure of G-quadruplex in the oncogene c-myc promoter and small ligands targeting the G-quadruplex. Firstly, the biological significance of c-myc G-quadruplex is introduced. Secondly, the structures of several c-myc G-quadruplexs are analyzed. Finally, the development of the small ligands targeting c-myc G-quadruplex is introduced, and the mechanism of the quadruplex-related drug candidate CX-3543 which has entered phase I clinical trial has been explored.