DNA minor groove binders inhibit the positive supercoiling activity of
Rad521-212.
A, structures of distamycin A, netropsin,
and pentamidine. B, topoisomerase I-mediated relaxation assay in the
presence of minor groove binding ligands. Increasing concentrations of the
ligands with or without 2 μm Rad521-212. Lanes
12, 24, and 36 show the addition of the ligands before E.
coli topoisomerase I. C, DNA binding activity of
Rad521-212 in the presence of the ligands. Negatively supercoiled
plasmid DNA (pGsat4, 3.2 kilobases) was used.