title: G-quadruplex binding ligands: from naturally occurring to rationally designed molecules.
abstract: Guanine-rich nucleic acid sequences are known to form G-quadruplex - four-stranded DNA or RNA structures stabilized by an array of Hoogsteen hydrogen bonds. G-quadruplex structures are involved in the modulation of gene expression at the transcription and translation levels. Accordingly, G-quadruplexes are considered as novel therapeutic targets for anticancer drug development. In this review, the authors provide a brief, up-to-date summary of G-quadruplex binding ligands, including naturally occurring molecules, synthetic compounds, and molecules identified by computational database screening. The key structural motifs of G-quadruplex binding ligands, that is, an aromatic core and basic side chains, are addressed in the context of how these molecules interact with G-quadruplex. A better understanding of these interactions would facilitate the rational design of ligands selective for DNA or RNA G-quadruplex.
authors.affiliation: School of Pharmacy, Sungkyunkwan University, Suwon, Korea.
authors.forename: Tuong
authors.initials: T
authors.lastname: Vy Thi Le
authors.forename: Sujin
authors.initials: S
authors.lastname: Han
authors.forename: Junghyun
authors.initials: J
authors.lastname: Chae
authors.forename: Hyun-Ju
authors.initials: HJ
authors.lastname: Park
mesh_terms: D000166:Acridines / Q000494:pharmacology; D000880:Anthraquinones / Q000494:pharmacology; D001599:Berberine / Q000494:pharmacology; D004247:DNA / Q000737:chemistry; D015195:Drug Design; D054856:G-Quadruplexes; D006801:Humans; D026121:Indole Alkaloids / Q000494:pharmacology; D008024:Ligands; D010080:Oxazoles / Q000494:pharmacology; D011166:Porphyrins / Q000494:pharmacology; D011804:Quinolines / Q000494:pharmacology; D012313:RNA / Q000737:chemistry
chemical_list: D000166:Acridines; D000880:Anthraquinones; D026121:Indole Alkaloids; D008024:Ligands; D010080:Oxazoles; D011166:Porphyrins; D011804:Quinolines; C431888:telomestatin; D001599:Berberine; C024015:cryptolepine; D012313:RNA; D004247:DNA