2. Academic Validation
  3. Evaluation of the interaction between long telomeric DNA and macrocyclic hexaoxazole (6OTD) dimer of a G-quadruplex ligand

Evaluation of the interaction between long telomeric DNA and macrocyclic hexaoxazole (6OTD) dimer of a G-quadruplex ligand

  • Molecules. 2013 Apr 12;18(4):4328-41. doi: 10.3390/molecules18044328.
Keisuke Iida 1,  Satoki Majima,  Takahiro Nakamura,  Hiroyuki Seimiya,  Kazuo Nagasawa
Affiliations

Affiliation

  • 1 Faculty of Technology, Tokyo University of Agriculture and Technology-TUAT, 2-24-16 Naka-cho, Koganei-shi, Tokyo 185-0031, Japan.
PMID: 23584054 DOI: 10.3390/molecules18044328
Abstract

Macrocyclic hexaoxazole dimer of L2H2-6OTD-dimer (3) was newly synthesized as a telomeric G-quadruplex (G4) ligand, and interaction with long telomeric DNAs telo48, 72, and 96 was evaluated by means of electrophoresis mobility shift assay, CD spectra analysis, and CD melting experiments. The L2H2-6OTD-dimer (3) interacted with the long telomeric DNAs by inducing anti-parallel type G4 structure of each unit of 24 bases, i.e., (TTAGGG)₄ sequences. Dimer 3 stabilizes long telomeric DNAs more efficiently than the corresponding monomer of L2H2-6OTD (2). It showed potent inhibitory activity against Telomerase, with an IC₅₀ value of 7.5 nm.

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