Recent Development of c-myc G-Quadruplex Ligands

Abstract

In this review, we summarize recent findings in the development of c-myc G-quadruplex ligands. Several features such as expanded aromatic rings, flexible molecules, dinuclear metal complexes, oligomers and G-quartet based ligands have been demonstrated to be advantageous for providing higher selectivity towards the c-myc G-quadruplex over duplex structures. High throughput screening methods including competition dialysis, G4 FID, FRET-based melting assay, direct ELISA and in silico virtual screening for analyzing the interaction between the ligands and the c-myc G-quadruplex are discussed. In particular, in silico virtual screening has been demonstrated to be a valuable means for the discovery of selective G-quadruplex ligands. Using this approach, ligands selective for the c-myc G-quadruplex have been successfully identified