Inhibition of Lysosomal Cysteine Proteases by a Series of Au(I) Complexes: A Detailed
Mechanistic Investigation
Shamila S. Gunatilleke
Amy M. Barrios
10.1021/jm060158f.s001
https://acs.figshare.com/articles/dataset/Inhibition_of_Lysosomal_Cysteine_Proteases_by_a_Series_of_Au_I_Complexes_A_Detailed_Mechanistic_Investigation/3073564
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 IC<sub>50</sub> values ranging
from 0.3 to 250 μM, depending on the substituents around the Au(I).
2006-06-29 00:00:00
series
cathepsin B
Inhibition
complex
250 μ M
derivative
Mechanistic InvestigationComplexes
IC 50 values
0.3
arthritis
substituent
inhibition
Lysosomal Cysteine Proteases
cathepsin family
inhibitor
Series
lysosomal cysteine proteases