title: G-quadruplex structures and their interaction diversity with ligands.
abstract: G-Quadruplexes are distinct nucleic acid secondary structures that are formed from G-rich DNA and RNA sequences; they are built around successive G-tetrads of Hoogsteen hydrogen-bonded guanine bases. The existence of G-quadruplex structures has been confirmed in the human telomere and genome, and their biological functions have been demonstrated. Thus, the prospect of using G-quadruplex structures as a novel target for drug design is important. This review focuses on structural polymorphism of G-quadruplexes on the basis of the classification of the strand number of the G-quadruplex formed and its interaction diversity with small molecules (G4-ligands) that display high affinity and, more importantly, selectivity. Also, we outlook some future challenges for G-quadruplex structure and ligand studies. Such information, together with the biological functions of for G-quadruplex, will be of crucial importance for the research and development of drugs that target G-quadruplexes formed from particular genes and human telomeres.
authors.affiliation: Lab of Chemical Biology & Molecular Drug Design, College of Pharmaceutical Science, Zhejiang University of Technology, 18 Chaowang Rd, Hangzhou, 310014 (China).
authors.forename: Sulin
authors.initials: S
authors.lastname: Zhang
authors.forename: Yanling
authors.initials: Y
authors.lastname: Wu
authors.forename: Wen
authors.initials: W
authors.lastname: Zhang
mesh_terms: D004247:DNA / Q000737:chemistry* / Q000187:drug effects; D015195:Drug Design; D054856:G-Quadruplexes / Q000187:drug effects; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D012313:RNA / Q000737:chemistry* / Q000187:drug effects; D054852:Small Molecule Libraries / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D008024:Ligands; D004364:Pharmaceutical Preparations; D054852:Small Molecule Libraries; D012313:RNA; D004247:DNA
keywords: G-Quadruplexes; drug design; interaction diversity; ligand effects; polymorphism