Directing topoisomerase I mediated DNA cleavage to specific sites by camptothecin tethered to minor- and major-groove ligands.
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).
Laboratoire de Biophysique, INSERM U201, UMR 8646 CNRS Muséum National d'Histoire Naturelle 43 rue Cuvier, 75231 Paris cedex 05, France, Fax: (+33) 1-40793705.
P B
PB
Arimondo
C
C
Bailly
A S
AS
Boutorine
V A
VA
Ryabinin
A N
AN
Syniakov
J S
JS
Sun
T
T
Garestier
C
C
Hélène
DNA cleavage; DNA recognition; antitumor agents; drug research; topoisomerase