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A Selective G-Quadruplex DNA-Stabilizing Ligand Based on a Cyclic Naphthalene Diimide Derivative

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  • معلومة اضافية
    • بيانات النشر:
      MDPI
    • الموضوع:
      2015
    • Collection:
      Kyushu Institute of Technology Academic Repository (Kyutacar) / 九州工業大学学術機関リポジトリ
    • نبذة مختصرة :
      A cyclic naphthalene diimide (cyclic NDI, 1), carrying a benzene moiety as linker chain, was synthesized and its interaction with G-quadruplex DNAs of a-core and a-coreTT as a human telomeric DNA, c-kit and c-myc as DNA sequence at promoter region, or thrombin-binding aptamer (TBA) studied based on UV-VIS and circular dichroism (CD) spectroscopic techniques, thermal melting temperature measurement, and FRET-melting assay. The circular dichroism spectra showed that 1 induced the formation of different types of G-quadruplex DNA structure. Compound 1 bound to these G-quadruplexes with affinities in the range of 106–107 M−1 order and a 2:1 stoichiometry. Compound 1 showed 270-fold higher selectivity for a-core than dsDNA with a preferable a-core binding than a-coreTT, c-kit, c-myc and TBA in the presence of K+, which is supported by thermal melting studies. The FRET-melting assay also showed that 1 bound preferentially to human telomeric DNA. Compound 1 showed potent inhibition against telomerase activity with an IC50 value of 0.9 μM and preferable binding to G-quadruplexes DNA than our previously published cyclic NDI derivative 3 carrying a benzene moiety as longer linker chain. ; Journal Article ; journal article
    • File Description:
      application/pdf
    • ISSN:
      1420-3049
    • Relation:
      https://doi.org/10.3390/molecules200610963; Molecules; 20; 10963; 10979; https://kyutech.repo.nii.ac.jp/record/4462/files/molecules-20-10963.pdf
    • Rights:
      Copyright (c) 2015 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/).
    • الرقم المعرف:
      edsbas.C2927179