1. On the mechanism of action of arsenoplatins: arsenoplatin-1 binding to a B-DNA dodecamer.
- Author
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Troisi, Romualdo, Tito, Gabriella, Ferraro, Giarita, Sica, Filomena, Massai, Lara, Geri, Andrea, Cirri, Damiano, Messori, Luigi, and Merlino, Antonello
- Subjects
ANTINEOPLASTIC agents ,CISPLATIN - Abstract
The reaction of Pt-based anticancer agents with arsenic trioxide affords robust complexes known as arsenoplatins. The prototype of this family of anticancer compounds is arsenoplatin-1 (AP-1) that contains an As(OH)
2 fragment linked to a Pt(II) moiety derived from cisplatin. Crystallographic and spectrometric studies of AP-1 binding to a B-DNA double helix dodecamer are presented here, in comparison with cisplatin and transplatin. Results reveal that AP-1, cisplatin and transplatin react differently with the DNA model system. Notably, in the AP-1/DNA systems, the Pt–As bond can break down with time and As-containing fragments can be released. These results have implications for the understanding of the mechanism of action of arsenoplatins. [ABSTRACT FROM AUTHOR]- Published
- 2024
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