title: Activity of rat cytosolic thioredoxin reductase is strongly decreased by trans-[bis(2-amino-5- methylthiazole)tetrachlororuthenate(III)]: first report of relevant thioredoxin reductase inhibition for a ruthenium compound.
abstract: A novel "Keppler type" ruthenium(III) compound trans-[bis(2-amino 5-methylthiazole)tetrachlororuthenate(III)] 1, of potential interest as an anticancer agent, was designed, synthesized, and characterized. Its interactions with various proteins were analyzed, including the selenoenzyme thioredoxin reductase, an emerging target for anticancer metallodrugs. The selective inhibition of the cytosolic form of this selenoenzyme was documented, this being the first report of significant thioredoxin reductase inhibition by a ruthenium compound.
authors.affiliation: Institute of Crystallography, Area della Ricerca di Roma 1 (CNR), Via Salaria Km 29,300, Montelibretti, Rome, Italy. pasquale.mura@ic.cnr.it
authors.forename: Pasquale
authors.initials: P
authors.lastname: Mura
authors.forename: Mercedes
authors.initials: M
authors.lastname: Camalli
authors.forename: Alberto
authors.initials: A
authors.lastname: Bindoli
authors.forename: Francesca
authors.initials: F
authors.lastname: Sorrentino
authors.forename: Angela
authors.initials: A
authors.lastname: Casini
authors.forename: Chiara
authors.initials: C
authors.lastname: Gabbiani
authors.forename: Maddalena
authors.initials: M
authors.lastname: Corsini
authors.forename: Piero
authors.initials: P
authors.lastname: Zanello
authors.forename: Maria Pia
authors.initials: MP
authors.lastname: Rigobello
authors.forename: Luigi
authors.initials: L
authors.lastname: Messori
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry; D003600:Cytosol / Q000201:enzymology*; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000737:chemistry; D008928:Mitochondria / Q000201:enzymology; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D051381:Rats; D054481:Thioredoxin Reductase 1 / Q000037:antagonists & inhibitors* / Q000737:chemistry; D054482:Thioredoxin Reductase 2 / Q000037:antagonists & inhibitors / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D007527:Isoenzymes; D009942:Organometallic Compounds; C526806:bis(2-amino-5-methylthiazole)tetrachlororuthenate(III); D054481:Thioredoxin Reductase 1; D054482:Thioredoxin Reductase 2; C516126:Txnrd1 protein, rat