期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 49, 期 13, 页码 3933-3937出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm060158f
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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).
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