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© Yang SI, Institut Pasteur
Publication : Angewandte Chemie (International ed. in English)

Directing topoisomerase I mediated DNA cleavage to specific sites by camptothecin tethered to minor- and major-groove ligands

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Angewandte Chemie (International ed. in English) - 01 Jan 2001

Arimondo PB, Bailly C, Boutorine AS, Ryabinin VA, Syniakov AN, Sun JS, Garestier T, Hélène C

Link to Pubmed [PMID] – 12203644

Angew. Chem. Int. Ed. Engl. 2001;40(16):3045-8

The covalent linkage of a hairpin polyamide, which binds in the minor groove, to camptothecin provides an efficient system to direct topoisomerase I mediated DNA cleavage to specific sites. These conjugates are equally as potent at targeting the enzyme to a single site in a DNA fragment as camptothecin conjugates of ligands that bind in the major groove (triplex-forming oligonucleotides).

https://www.ncbi.nlm.nih.gov/pubmed/12203644