title: Rational design of an organometallic glutathione transferase inhibitor.
abstract: Double trouble: A hybrid organic-inorganic (organometallic) inhibitor was designed to target glutathione transferases. The metal center is used to direct protein binding, while the organic moiety acts as the active-site inhibitor (see picture). The mechanism of inhibition was studied using a range of biophysical and biochemical methods.
authors.affiliation: Institut des Sciences et Ingénierie Chimiques, Ecole Polytechnique Fédérale de Lausanne, 1015 Lausanne, Switzerland.
authors.forename: Wee Han
authors.initials: WH
authors.lastname: Ang
authors.forename: Lorien J
authors.initials: LJ
authors.lastname: Parker
authors.forename: Anastasia
authors.initials: A
authors.lastname: De Luca
authors.forename: Lucienne
authors.initials: L
authors.lastname: Juillerat-Jeanneret
authors.forename: Craig J
authors.initials: CJ
authors.lastname: Morton
authors.forename: Mario
authors.initials: M
authors.lastname: Lo Bello
authors.forename: Michael W
authors.initials: MW
authors.lastname: Parker
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Dyson
mesh_terms: D018360:Crystallography, X-Ray; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D005982:Glutathione Transferase / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism*; D008958:Models, Molecular; D015394:Molecular Structure; D009154:Mutation / Q000235:genetics; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D009942:Organometallic Compounds; D005982:Glutathione Transferase