Recognition and cleavage of DNA by rebeccamycin- or benzopyridoquinoxalineconjugated of triple helix-forming oligonucleotides

Citation
Pb. Arimondo et al., Recognition and cleavage of DNA by rebeccamycin- or benzopyridoquinoxalineconjugated of triple helix-forming oligonucleotides, BIO MED CH, 8(4), 2000, pp. 777-784
Citations number
34
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
09680896 → ACNP
Volume
8
Issue
4
Year of publication
2000
Pages
777 - 784
Database
ISI
SICI code
0968-0896(200004)8:4<777:RACODB>2.0.ZU;2-X
Abstract
Indolocarbazole and benzopyridoquinoxaline derivatives have been shown to h ave anti-tumor activity and to stimulate DNA topoisomerase I-mediated cleav age. Two indolocarbazole compounds (R-6 and R-95) and one benzopyridoquinox aline derivative (BPQ(1256)) were covalently attached to the 3'-end of a 16 mer triple helix-forming oligonucleotide (TFO). These conjugates bind to DN A with a higher affinity than the unsubstituted oligonucleotides. Furthermo re, they induce topoisomerase I-mediated and tripler-directed DNA cleavage in a sequence-specific manner. (C) 2000 Elsevier Science Ltd. All rights re served.