Abstract
NETGA is an hybrid derivative which possesses an intercalating heterocyclic nucleus related to amsacrine and a minor groove binding squeletton related to netropsin. Cellular uptake of this drug has been studied by Electron Spin Resonance (ESR) spectroscopy using a spin-label derivative of NETGA (SL-NETGA). ESR determination of the kinetics of the drug repartition between the cytoplasm and nucleus showed that NETGA accumulated very rapidly and predominantly in the nucleus. Analysis of the anisotropic ESR spectra recorded in the nuclear compartment are in agreement with a strong binding of the drug to the DNA besides confirmed by a maximum ΔTm of 12°C between the spin-label compound-DNA complex and the DNA alone.
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