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Hampshire, Andrew J., Rusling, David A., Bryan, Stephanie, Paumier, David, Dawson, Simon J., Malkinson, John P., Searcey, Mark 
ORCID: https://orcid.org/0000-0003-2273-8949 and Fox, Keith R.
(2008)
DNA binding by analogues of the bifunctional intercalator TANDEM.
Biochemistry, 47 (30).
pp. 7900-7906.
Abstract
We have used DNase I footprinting to study the binding strength and DNA sequence selectivity of novel derivatives of the quinoxaline bis-intercalator TANDEM. Replacing the valine residues in the cyclic octadepsipeptide with lysines does not affect the selectivity for TpA but leads to a 50-fold increase in affinity. In contrast, replacing both of the quinoxaline chromophores with naphthalene rings abolishes binding, while changing a single ring decreases the affinity, and footprints are observed at only the best binding sites (especially TATATA). By using fragments with different lengths of [(AT)n], we demonstrate that these ligands bind best to the center of the longer (AT)n tracts.
| Item Type: | Article |
|---|---|
| Faculty \ School: | Faculty of Science > School of Pharmacy |
| UEA Research Groups: | Faculty of Science > Research Groups > Medicinal Chemistry (former - to 2017) Faculty of Science > Research Groups > Chemical Biology and Medicinal Chemistry (former - to 2021) |
| Depositing User: | Rachel Smith |
| Date Deposited: | 17 Mar 2011 14:21 |
| Last Modified: | 12 Jan 2023 17:30 |
| URI: | https://ueaeprints.uea.ac.uk/id/eprint/26560 |
| DOI: | 10.1021/bi800573p |
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