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

Basic Information

ID: ALA1146328

Journal: Bioorg Med Chem Lett

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

Authors: McKnight RE, Gleason AB, Keyes JA, Sahabi S.

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.

CiteXplore: 17157016

DOI: 10.1016/j.bmcl.2006.11.038

Patent ID: