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Investigations into the DNA-binding mode of doxorubicinone

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Abstract

Cancer treatment is one of the major challenges facing the modern biomedical profession. Development of new small-molecule chemotherapeutics requires an understanding of the mechanism of action for these treatments, as well as the structure–activity relationship. Study of the well-known DNA-intercalating agent, doxorubicin, and its aglycone, doxorubicinone, was undertaken using a variety of spectroscopic and calorimetric techniques. It was found that, despite conservation of the planar, aromatic portion of doxorubicin, the agylcone does not intercalate; it instead likely binds to the DNA minor-groove.

Graphical abstract: Investigations into the DNA-binding mode of doxorubicinone

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Publication details

The article was received on 21 Sep 2018, accepted on 31 Oct 2018 and first published on 31 Oct 2018


Article type: Paper
DOI: 10.1039/C8OB02344A
Citation: Org. Biomol. Chem., 2018, Advance Article
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    Investigations into the DNA-binding mode of doxorubicinone

    S. S. Tartakoff, J. M. Finan, E. J. Curtis, H. M. Anchukaitis, D. J. Couture and S. Glazier, Org. Biomol. Chem., 2018, Advance Article , DOI: 10.1039/C8OB02344A

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