Chemical conversion of cisplatin and carboplatin with histidine in a model protein crystallized under sodium iodide conditions

Crystals of HEWL with cisplatin and HEWL with carboplatin grown in sodium iodide conditions both show a partial chemical transformation of cisplatin or carboplatin to a transiodoplatin (PtI₂X₂) form. The binding is only at the N^δ atom of His15. A further Pt species (PtI₃X) is also seen, in both cases bound in a crevice between symmetry-related protein molecules.

The binding of platinum hexahalides (Cl, Br and I) to hen egg-white lysozyme and the chemical transformation of the PtI₆ octahedral complex to a PtI₃ moiety bound to His15

The platinum hexahalides have an octahedral arrangement of six halogen atoms bound to a Pt centre, thus having an octahedral shape that could prove to be useful in interpreting poor electron-density maps. In a detailed characterization, PtI₆ chemically transformed to a square-planar PtI₃ complex bound to the N^δ atom of His15 of HEWL was also observed, which was not observed for PtBr₆ or PtCl₆.

Carboplatin binding to histidine

An X-ray crystal structure showing the binding of purely carboplatin to histidine in a model protein has finally been obtained. This required extensive crystallization trials and various novel crystal structure analyses.