Hampshire, A..J., Rusling, D.A., Bryan, S., Paumier, D., Dawson, S.J., Malkinson, J.P., Searcey, M. and Fox, K.R. (2008) DNA binding by analogues of the bifunctional intercalator TANDEM. Biochemistry, 47 (30). pp. 7900-7906. 10.1021/bi800573p.
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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.
|Departments, units and centres:||Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry|
|Journal or Publication Title:||Biochemistry|
|Deposited By:||Library Staff|
|Deposited On:||16 Mar 2012 09:48|
|Last Modified:||16 Mar 2012 09:48|
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