On the mechanism of action of arsenoplatins: arsenoplatin-1 binding to a B-DNA dodecamer.
Troisi, R., Tito, G., Ferraro, G., Sica, F., Massai, L., Geri, A., Cirri, D., Messori, L., Merlino, A.(2024) Dalton Trans 53: 3476-3483
- PubMed: 38270175 
- DOI: https://doi.org/10.1039/d3dt04302a
- Primary Citation of Related Structures:  
8C62, 8C63, 8C64, 8RI3, 8RI5 - PubMed 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.
Organizational Affiliation: 
Department of Chemical Sciences, University of Naples Federico II, Complesso Universitario di Monte Sant'Angelo, via Cintia, 80126, Naples, Italy. [email protected].