Single molecule brightness analysis for determination of anticancer drugs interactions with DNA

Zhou Y., Bielec K., Pasitsuparoad,P., Holyst R.

The Analyst (2020) DOI: 10.1039/d0an01108h


rysAnthracyclines are one of the most studied anticancer drugs approved for medical treatment. The equilibrium constant (K) of the reaction between these drugs with DNA in both in vitro and in vivo experiments lacks consensus. The K values vary from 104 up to 108 M−1, which suggest a 1000-fold error in determining the effective concentration needed to form the drug–DNA complex. Until 2014, only one study by García [J. Phys. Chem. B, 2014, 118, 1288–1295] showed that the binding of anthracycline representative doxorubicin occurs in two reactions. We support this result by brightness analysis at a single molecular level for the four most common anthracyclines: doxorubicin, daunorubicin, epirubicin, and idarubicin.

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This project has received funding from the European Union’s Horizon 2020 research and innovation programme under the Marie Skłodowska-Curie grant agreement No. 711859.