Premium
Directing Topoisomerase I Mediated DNA Cleavage to Specific Sites by Camptothecin Tethered to Minor‐ and Major‐Groove Ligands
Author(s) -
Arimondo Paola B.,
Bailly Christian,
Boutorine Alexandre S.,
Ryabinin Vladimir A.,
Syniakov Alexandre N.,
Sun JianSheng,
Garestier Thérèse,
Hélène Claude
Publication year - 2001
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/1521-3773(20010817)40:16<3045::aid-anie3045>3.0.co;2-a
Subject(s) - camptothecin , minor groove , cleavage (geology) , topoisomerase , dna , chemistry , groove (engineering) , microbiology and biotechnology , biology , biochemistry , materials science , fracture (geology) , metallurgy , paleontology
The covalent linkage of a hairpin polyamide , which binds in the minor groove, to camptothecin (see picture) 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).