title: The recognition of higher-order G-quadruplex by chiral cyclic-helicene molecules.
abstract: The G-quadruplex structures represent a new class of molecular targets for DNA-interactive compounds that might be useful for targeting telomeres. Here we describe a study on the structure-based design of cyclic helicenes displaying chiral and steric selection in binding to higher-order G-quadruplexes. We propose a new ligand-binding site for G-quadruplex-binding compounds. These results provide proof of concept for small molecule inhibitors of telomerase associated with higher-order G-quadruplex structures.
authors.affiliation: Department of Chemistry, Graduate School of Science, Kyoto University, Sakyo, Kyoto 606-8502, Japan.
authors.forename: Yan
authors.initials: Y
authors.lastname: Xu
authors.forename: Shinya
authors.initials: S
authors.lastname: Yamazaki
authors.forename: Hideji
authors.initials: H
authors.lastname: Osuga
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Sugiyama
mesh_terms: D001665:Binding Sites; D002942:Circular Dichroism; D004247:DNA / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000737:chemistry*; D054856:G-Quadruplexes; D006801:Humans; D008024:Ligands; D009838:Oligodeoxyribonucleotides / Q000737:chemistry; D011083:Polycyclic Compounds / Q000737:chemistry*; D013050:Spectrometry, Fluorescence; D013237:Stereoisomerism; D019098:Telomerase / Q000037:antagonists & inhibitors*; D016615:Telomere / Q000737:chemistry*
chemical_list: D004791:Enzyme Inhibitors; D008024:Ligands; D009838:Oligodeoxyribonucleotides; D011083:Polycyclic Compounds; C031660:helicenes; D004247:DNA; D019098:Telomerase