title: Identifying and characterizing the biological targets of metallotherapeutics: Two approaches using Au(I)-protein interactions as model systems.
abstract: A significant challenge in the field of medicinal inorganic chemistry is the identification of biological targets of metal-based drugs and the characterization of the metal-biomolecule adducts. A classic example is Au(I), which has long been used to treat rheumatoid arthritis despite a poor understanding of its biological targets due to the lability, reactivity, and "spectroscopic silence" that are characteristic of Au(I). Here, we report two qualitative methods for characterizing Au(I)-protein adducts: a thiol-reactive probe that facilitates the identification of biological cysteine-Au(I) adducts and a photoreactive Au(I) complex that produces a covalent bond between the Au(I) complex and the biomolecule.
authors.affiliation: University of Southern California, Los Angeles, CA 90089, USA.
authors.forename: Mark R
authors.initials: MR
authors.lastname: Karver
authors.forename: Amy M
authors.initials: AM
authors.lastname: Barrios
mesh_terms: D000818:Animals; D001310:Auranofin / Q000378:metabolism / Q000627:therapeutic use; D001665:Binding Sites; D002417:Cattle; D006046:Gold / Q000378:metabolism* / Q000627:therapeutic use*; D006801:Humans; D010206:Papain / Q000378:metabolism; D011485:Protein Binding; D013267:Stilbenes / Q000378:metabolism
chemical_list: C090885:4-acetamido-4'-((iodoacetyl)amino)stilbene-2,2'-disulfonate; D013267:Stilbenes; D001310:Auranofin; D006046:Gold; D010206:Papain