title: Stabilizing G-quadruplex DNA by methylazacalix[n]pyridine through shape-complementary interaction.
abstract: It is found that G-quadruplexes have important functions in biological systems, such as gene expression. Molecules which can stabilize the G-quadruplex structure may have potential application in regulating the expression of gene. A series of methylazacalix[n]pyridine (n=4, 6, 7, 8, 9) has been tested to stabilize the intermolecular human telomeric G-quadruplex (T12 and H12), intramolecular TBA, c-kit and bcl-2 G-quadruplex by CD denaturation experiments. The results showed that only methylazacalix[6]pyridine (MACP6) can stabilize the intermolecular G-quadruplex formed from the 12bp human telomere. Further studies evidenced that the shape-complementary binding mode was what contributed to the interaction between MACP6 and T12 G-quadruplex.
authors.affiliation: Beijing National Laboratory for Molecular Sciences, Center for Molecular Sciences, State Key Laboratory for Structural Chemistry of Unstable and Stable Species, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, PR China.
authors.forename: Ai-Jiao
authors.initials: AJ
authors.lastname: Guan
authors.affiliation: Department of Chemistry, Renmin University of China, Beijing 100872, PR China.
authors.forename: Meng-Jie
authors.initials: MJ
authors.lastname: Shen
authors.affiliation: Department of Chemistry, Tsinghua University, Beijing 100084, PR China.
authors.forename: En-Xuan
authors.initials: EX
authors.lastname: Zhang
authors.affiliation: Beijing National Laboratory for Molecular Sciences, Center for Molecular Sciences, State Key Laboratory for Structural Chemistry of Unstable and Stable Species, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, PR China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Li
authors.affiliation: Beijing National Laboratory for Molecular Sciences, Center for Molecular Sciences, State Key Laboratory for Structural Chemistry of Unstable and Stable Species, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, PR China.
authors.forename: Li-Xia
authors.initials: LX
authors.lastname: Wang
authors.affiliation: Department of Chemistry, Renmin University of China, Beijing 100872, PR China. Electronic address: xulj@chem.ruc.edu.cn.
authors.forename: Li-Jin
authors.initials: LJ
authors.lastname: Xu
authors.affiliation: Beijing National Laboratory for Molecular Sciences, Center for Molecular Sciences, State Key Laboratory for Structural Chemistry of Unstable and Stable Species, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, PR China. Electronic address: jfxiang@iccas.ac.cn.
authors.forename: Jun-Feng
authors.initials: JF
authors.lastname: Xiang
authors.affiliation: Beijing National Laboratory for Molecular Sciences, Center for Molecular Sciences, State Key Laboratory for Structural Chemistry of Unstable and Stable Species, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, PR China. Electronic address: tangyl@iccas.ac.cn.
authors.forename: Ya-Lin
authors.initials: YL
authors.lastname: Tang
mesh_terms: D047250:Calixarenes / Q000494:pharmacology*; D002942:Circular Dichroism; D004247:DNA / Q000737:chemistry*; D005079:Excipients / Q000494:pharmacology*; D054856:G-Quadruplexes / Q000187:drug effects*; D006801:Humans; D062105:Molecular Docking Simulation; D009691:Nucleic Acid Denaturation / Q000187:drug effects; D016615:Telomere / Q000737:chemistry / Q000187:drug effects*
chemical_list: D005079:Excipients; C570637:methylazacalix(6)pyridine; D047250:Calixarenes; D004247:DNA
keywords: Circular dichroism; G-quadruplexes; Methylazacalix[n]pyridine; Molecular docking; Stabilize