1. Investigations into the DNA-binding mode of doxorubicinone
- Author
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Haley M Anchukaitis, Ellis J Curtis, Samantha Glazier, Danielle J Couture, Samuel Steucek Tartakoff, and Jennifer M Finan
- Subjects
Naphthacenes ,Molecular Conformation ,Calorimetry ,010402 general chemistry ,01 natural sciences ,Biochemistry ,Molecular conformation ,Structure-Activity Relationship ,chemistry.chemical_compound ,Doxorubicinone ,medicine ,Humans ,Structure–activity relationship ,Doxorubicin ,Physical and Theoretical Chemistry ,Binding Sites ,010405 organic chemistry ,Organic Chemistry ,DNA, Neoplasm ,Combinatorial chemistry ,Intercalating Agents ,0104 chemical sciences ,Cancer treatment ,Aglycone ,Mechanism of action ,chemistry ,medicine.symptom ,DNA ,medicine.drug - 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.
- Published
- 2019
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