Characteristics
PNU-159682, a metabolite of the anthracycline neomycin metabolite, is a DNA topoisomerase I (TopoI) inhibitor with excellent cytotoxicity. It is a more potent and tolerable ADC cytotoxin than doxorubicin in ADC synthesis.
Uses
PNU-159682 can be used in EDV nanocell technology to overcome drug resistance.
Biological Activity
PNU-159682, an active nemorubicin metabolite, is a highly potent anthracycline toxin th at retains antitumor activity in vivo. Similarly to other anthracyclines PNU-159682 intercalates between the CG base pairs of DNA, but the stability of the complexes is much higher.