Binding of 2-Hydroxypyridine-N-oxide on Dicopper(II) Centers: Insights into Tyrosinase Inhibition Mechanism by Transition-State Analogs

作者：Peyroux Eugenie; Ghattas Wadih; Hardre Renaud; Giorgi Michel; Faure Bruno; Simaan A Jalila; Belle Catherine^*; Reglier Marius

来源：Inorganic Chemistry, 2009, 48(23): 10874-10876.

DOI：10.1021/ic901593x

2-Hydroxypyridine-N-oxide (HOPNO) is described as a new and efficient transition-state analog (TS-analog) inhibitor for the mushroom tyrosinase with an IC(50) = 1.16 mu M and a K(I) = 1.8 mu M. Using the binuclear copper(II) complex [Cu(2)(BPMP)(mu-OH)](ClO(4))(2) (2) known as a functional model for the tyrosinase catecholase activity, we isolated and fully characterized a 1:1 (2)/OPNO adduct in which the HOPNO is deprotonated and chelates only one Cu-atom of the binuclear site in a bidentate mode. On the basis of these results, a structural model for the tyrosinase inhibition by HOPNO is proposed.

• 出版日期2009-12-7