作者: Luigi Messori , Maria Agostina Cinellu , Antonello Merlino
DOI: 10.1021/ML500231B
关键词: Prodrug 、 Chemistry 、 Hydrolase 、 Stereochemistry 、 Protein recognition 、 Model protein 、 Adduct 、 Lysozyme 、 Ligand 、 Metal
摘要: The structure of the adduct formed in reaction between Aubipyc, a cytotoxic organogold(III) compound, and model protein hen egg white lysozyme (HEWL) has been solved by X-ray crystallography. It emerges that after interaction with HEWL, undergoes reduction gold(III) center followed detaching cyclometalated ligand; resulting naked gold(I) ion is found bound to at Gln121. A direct comparison present those previously for adducts other compounds demonstrates coordinated ligands play key role protein–metallodrug recognition process. Structural data support view gold(III)-based antitumor prodrugs are activated through metal reduction.