Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 13, Pages 3933-3937Publisher
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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