Inhibition of lysosomal cysteine proteases by a series of Au(I) complexes: A detailed mechanistic investigation
Inhibition of lysosomal cysteine proteases by a series of Au(I) complexes: A detailed mechanistic investigation
复制标题
DOI：
10.1021/jm060158f
复制
发表时间：
2006-06-29
影响因子：
7.3
通讯作者：
Barrios, Amy M.
中科院分区：
文献类型：
--
作者：
Gunatilleke, Shamila S.;Barrios, Amy M.
尽管金的精确生物学靶点尚不清楚，但金 (I) 复合物长期以来一直用于治疗类风湿性关节炎。 Au(I) 的一个有趣的治疗靶点是溶酶体半胱氨酸蛋白酶的组织蛋白酶家族。在这里，我们介绍了一种已知的 Au(I) 基药物和一系列衍生物对组织蛋白酶 B 的抑制作用。研究的复合物是可逆的竞争性抑制剂，IC50 值范围为 0.3 至 250 μM，具体取决于 Au(I) 周围的取代基。
Complexes of gold( I) have long been used to treat rheumatoid arthritis although the precise biological targets of gold are not well understood. One intriguing therapeutic target of Au( I) is the cathepsin family of lysosomal cysteine proteases. Here, we present the inhibition of cathepsin B by a known Au( I)-based drug and a series of derivatives. The complexes investigated were reversible, competitive inhibitors with IC50 values ranging from 0.3 to 250 mu M, depending on the substituents around the Au( I).