Published September 12, 2001
| Supplemental Material
Journal Article
Open
Sequence-specific trapping of topoisomerase I by DNA binding polyamide-camptothecin conjugates
- Creators
- Wang, Clay C. C.
- Dervan, Peter B.
Abstract
Hairpin pyrrole−imidazole polyamides are synthetic ligands that bind in the minor groove of DNA with affinities and specificities comparable to those of DNA binding proteins. Three polyamide−camptothecin conjugates 1−3 with linkers varying in length between 7, 13, and 18 atoms were synthesized to trap the enzyme Topoisomerase I and induce cleavage at predetermined DNA sites. One of these, polyamide−camptothecin conjugate 3 at nanomolar concentration (50 nM) in the presence of Topo I (37 °C), induces DNA cleavage between three and four base pairs from the polyamide binding site in high yield (77%).
Additional Information
© 2001 American Chemical Society. Received February 13, 2001; Publication Date (Web): August 16, 2001. We are grateful to the National Institutes of Health (GM-27681) for research support and a traineeship award (GM-08501) to C.C.C.W.Attached Files
Supplemental Material - ja010392p_s.pdf
Files
ja010392p_s.pdf
Files
(165.9 kB)
Name | Size | Download all |
---|---|---|
md5:ac904d2768a483ac06c3b136f5824858
|
165.9 kB | Preview Download |
Additional details
- Eprint ID
- 66821
- DOI
- 10.1021/ja010392p
- Resolver ID
- CaltechAUTHORS:20160510-082725087
- GM-27681
- NIH
- GM-08501
- NIH Predoctoral Fellowship
- Created
-
2016-05-18Created from EPrint's datestamp field
- Updated
-
2021-11-11Created from EPrint's last_modified field