DNA binding by analogues of the bifunctional intercalator TANDEM

Hampshire, Andrew J., Rusling, David A., Bryan, Stephanie, Paumier, David, Dawson, Simon J., Malkinson, John P., Searcey, Mark and Fox, Keith R. (2008) DNA binding by analogues of the bifunctional intercalator TANDEM. Biochemistry, 47 (30). pp. 7900-7906.

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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 (former - to 2024)
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:	06 Feb 2025 02:26
URI:	https://ueaeprints.uea.ac.uk/id/eprint/26560
DOI:	10.1021/bi800573p

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