Inhibition of lysosomal cysteine proteases by a series of Au(I) complexes

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Subtitle: A detailed mechanistic investigation
Author list: Gunatilleke SS, Barrios AM
Publisher: American Chemical Society
Publication year: 2006
Volume number: 49
Issue number: 13
Start page: 3933
End page: 3937
Number of pages: 5
ISSN: 0022-2623
Languages: English-Great Britain (EN-GB)


Abstract

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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Last updated on 2019-23-08 at 11:15