Cisplatin Encapsulation within the Ferritin Nanocage: A High-Resolution Crystallographic Study

CDDP-encapsulated AFt appears to be an ideal nanocarrier for CDDP delivery to target sites, as it possesses a high biocompatibility and can be internalized by receptor mediated endocytosis thus carrying the drug to tumor tissue with higher selectivity than free CDDP.

N Pontillo et al., Chem. Commun., 2016
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Cisplatin (CDDP) can be encapsulated within the central cavity of reconstituted (apo)ferritin, (A)Ft, to form a drug-loaded protein of potential great interest for targeted cancer treatments. In this study, the interactions occurring between cisplatin and native horse spleen Ft in CDDP-encapsulated AFt  are  investigated  by  high-resolution  X-ray crystallography. A protein bound Pt center is unambiguously identified in AFt subunits by comparative analysis of difference Fourier electron density maps and of anomalous dispersion data. Indeed, a [Pt(NH3)2 H2O]2+ fragment is found coordinated to the His132 residues located onthe inner surface of the large AFt spherical cage.

 Remarkably, Pt binding does not alter the overall physicochemical features (shape, volume, polarity/hydrophobicity and electrostatic potential) of AFt nanocage outer surface.

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Cisplatin Encapsulation within the Ferritin Nanocage: A High-Resolution Crystallographic Study;
N Pontillo, F Pane, L Messori, A Amoresano, and A Merlino,
Chem. Commun., 2016;
doi:10.1039/C5CC10365G

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