Department of Chemical Sciences, University of Naples Federico II , Napoli, Italy.
Inorg Chem. 2013 Oct 7;52(19):10714-6. doi: 10.1021/ic401494v. Epub 2013 Sep 16.
A Raman-assisted crystallographic study on the adduct between AziRu, a Ru(III) complex with high antiproliferative activity, and RNase A is presented. The protein structure is not perturbed significantly by the Ru label. The metal coordinates to ND atoms of His105 or of His119 imidazole rings, losing all of its original ligands but retaining octahedral, although distorted, coordination geometry. The AziRu binding inactivates the enzyme, suggesting that its antitumor action can be exerted by a mechanism of competitive inhibition.
本文报道了具有高抗增殖活性的 Ru(III) 配合物 AziRu 与 RNase A 加合物的拉曼辅助晶体学研究。该研究表明，Ru 标记并未显著扰乱蛋白质结构。金属与 His105 或 His119 咪唑环的 ND 原子配位，失去了所有原始配体，但保留了八面体结构，尽管配位几何形状发生了扭曲。AziRu 的结合使酶失活，这表明其抗肿瘤作用可能通过竞争性抑制机制发挥。
