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Cisplatin Encapsulation within the Ferritin Nanocage: A High-Resolution Crystallographic Study
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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. |
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. Retrieve Article
Cisplatin Encapsulation within the Ferritin Nanocage: A High-Resolution Crystallographic Study;
Chem. Commun., 2016; |