title: Metal-based compounds as prospective antileishmanial agents: inhibition of trypanothione reductase by selected gold complexes.
abstract: Picking a fight with parasites! Trypanothione reductase (TR) is a validated drug target for the development of antileishmanial agents. A group of structurally diverse gold-containing compounds was evaluated in vitro for TR inhibition. A number of compounds exhibited potent activity and deserve further pharmacological evaluation.
authors.affiliation: Institute of Molecular Biology & Pathology; National Research Council (CNR); Institute Pasteur Fondazione Cenci Bolognetti; Department of Biochemical Sciences, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome (Italy). gianni.colotti@uniroma1.it.
authors.forename: Gianni
authors.initials: G
authors.lastname: Colotti
authors.forename: Andrea
authors.initials: A
authors.lastname: Ilari
authors.forename: Annarita
authors.initials: A
authors.lastname: Fiorillo
authors.forename: Paola
authors.initials: P
authors.lastname: Baiocco
authors.forename: Maria Agostina
authors.initials: MA
authors.lastname: Cinellu
authors.forename: Laura
authors.initials: L
authors.lastname: Maiore
authors.forename: Federica
authors.initials: F
authors.lastname: Scaletti
authors.forename: Chiara
authors.initials: C
authors.lastname: Gabbiani
authors.forename: Luigi
authors.initials: L
authors.lastname: Messori
mesh_terms: D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D020134:Catalytic Domain; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006046:Gold / Q000737:chemistry*; D007700:Kinetics; D007891:Leishmania / Q000187:drug effects / Q000201:enzymology; D062105:Molecular Docking Simulation; D009247:NADH, NADPH Oxidoreductases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011485:Protein Binding
chemical_list: D000981:Antiprotozoal Agents; D056831:Coordination Complexes; D004791:Enzyme Inhibitors; D006046:Gold; D009247:NADH, NADPH Oxidoreductases; C049608:trypanothione reductase
keywords: Leishmania; antiprotozoal agents; gold; inhibitors; trypanothione reductase