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Volumn 17, Issue 9, 2007, Pages 2515-2522

New highly hydrosoluble and not self-aggregated perylene derivatives with three and four polar side-chains as G-quadruplex telomere targeting agents and telomerase inhibitors

Author keywords

G quadruplex; Hydrosoluble perylene derivatives; Telomerase inhibitors

Indexed keywords

PERYLENE DERIVATIVE; TELOMERASE; TELOMERASE INHIBITOR; UNCLASSIFIED DRUG;

EID: 33947713244     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.02.021     Document Type: Article
Times cited : (46)

References (50)
  • 32
    • 33947715813 scopus 로고    scopus 로고
    • note
    • 17 The binding site was defined as the external 3′ G-quartet plane. Initially 200 ligand orientations were randomly centred on the G-quadruplex structure, charges were not considered and the complexes were minimized for 500 steps. The 75 lowest energy structures were then subjected to simulated annealing, then 500 steps of minimization were followed by molecular dynamics over a period of 10 ps. The energies of the resulting structures were then minimized.
  • 38
    • 33947716669 scopus 로고    scopus 로고
    • note
    • 24 was purchased from Pierce, as a 1 mM solution in MES buffer.
  • 40
    • 33947721056 scopus 로고    scopus 로고
    • note
    • 27 or DMSO. Samples were left equilibrating for half an hour before starting the experiment.
  • 46
    • 33947728796 scopus 로고    scopus 로고
    • note
    • Radio-labelled TSG4 oligonucleotide (5′-GGGATTGGGATTGGGATTGGGTT-3′) was heated at 95 °C for 10 min and quickly cooled in ice, at a concentration of 12 μM. It was then incubated for 2 h at 30 °C in MES-KCl buffer (10 mM MES, pH 6.5, and 5 mM KCl) in the presence of different drug concentrations and with no drug. Complexes and structures formed after incubation were studied by native PAGE (15% polyacrylamide gel, TBE 0.5×, KCl 20 mM, run overnight at room temperature). In all electrophoresis runs, the G-quadruplex induction by PIPER (20 μM) was also reported as a useful standard to assign the electrophoresis bands to different DNA conformations. Percentage of ss-DNA represents the ratio between the intensity of the relative band on the electrophoresis gel and the total amount of DNA, obtained by Instant Imager (Packard).
  • 48
    • 33947731226 scopus 로고    scopus 로고
    • note
    • 31


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.