Gunatilleke Shamila S, Barrios Amy M
Department of Chemistry, University of Southern California, Los Angeles, California 90089, USA.
J Med Chem. 2006 Jun 29;49(13):3933-7. doi: 10.1021/jm060158f.
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 microM, depending on the substituents around the Au(I).
长期以来，金（I）配合物一直被用于治疗类风湿性关节炎，尽管金的确切生物学靶点尚未完全明确。金（I）一个引人关注的治疗靶点是溶酶体半胱氨酸蛋白酶组织蛋白酶家族。在此，我们展示了一种已知的基于金（I）的药物及其一系列衍生物对组织蛋白酶B的抑制作用。所研究的配合物是可逆的竞争性抑制剂，其IC50值在0.3至250微摩尔之间，具体取决于金（I）周围的取代基。
