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© Yang SI, Institut Pasteur
Publication : Bioorganic & medicinal chemistry

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

Team: Epigenetic Chemical Biology
Member: Paola Arimondo
Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Bioorganic & medicinal chemistry - 01 Apr 2000

Arimondo PB, Moreau P, Boutorine A, Bailly C, Prudhomme M, Sun JS, Garestier T, Hélène C

Link to Pubmed [PMID] – 10819166

Bioorg. Med. Chem. 2000 Apr;8(4):777-84

Indolocarbazole and benzopyridoquinoxaline derivatives have been shown to have anti-tumor activity and to stimulate DNA topoisomerase I-mediated cleavage. Two indolocarbazole compounds (R-6 and R-95) and one benzopyridoquinoxaline derivative (BPQ(1256)) were covalently attached to the 3′-end of a 16mer triple helix-forming oligonucleotide (TFO). These conjugates bind to DNA with a higher affinity than the unsubstituted oligonucleotides. Furthermore, they induce topoisomerase I-mediated and triplex-directed DNA cleavage in a sequence-specific manner.