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American Chemical Society, ACS Medicinal Chemistry Letters, 10(5), p. 1110-1113, 2014

DOI: 10.1021/ml500231b

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Protein Recognition of Gold-Based Drugs: 3D Structure of the Complex Formed When Lysozyme Reacts with Aubipyc

Journal article published in 2014 by Luigi Messori, Maria Agostina Cinellu, Antonello Merlino ORCID
This paper is available in a repository.
This paper is available in a repository.

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Abstract

The structure of the adduct formed in the reaction between Aubipy(c), a cytotoxic organogold(III) compound, and the model protein hen egg white lysozyme (HEWL) has been solved by X-ray crystallography. It emerges that Aubipy(c), after interaction with HEWL, undergoes reduction of the gold(III) center followed by detaching of the cyclometalated ligand; the resulting naked gold(I) ion is found bound to the protein at Gln121. A direct comparison between the present structure and those previously solved for the lysozyme adducts with other gold(III) compounds demonstrates that coordinated ligands play a key role in the protein-metallodrug recognition process. Structural data support the view that gold(III)-based antitumor prodrugs are activated through metal reduction.