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Bioorg Med Chem Lett. 2007 Feb 15;17(4):1013-7. Epub 2006 Nov 16.

Binding mode and affinity studies of DNA-binding agents using topoisomerase I DNA unwinding assay.

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1
Department of Chemistry, State University of New York at Geneseo, 1 College Circle, Geneseo, NY 14454, USA. mcknight@geneseo.edu

Abstract

A topoisomerase I DNA unwinding assay has been used to determine the relative DNA-binding affinities of a model pair of homologous naphthalene diimides. Binding affinity data were corroborated using calorimetric (ITC) and spectrophotometric (titration and T(m)) studies, with substituent size playing a significant role in binding. The assay was also used to investigate the mode of binding adopted by several known DNA-binding agents, including SYBR Green and PicoGreen. Some of the compounds exhibited unexpected binding modes.

PMID:
17157016
DOI:
10.1016/j.bmcl.2006.11.038
[Indexed for MEDLINE]
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