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J Enzyme Inhib Med Chem. 2014 Aug;29(4):538-46. doi: 10.3109/14756366.2013.823957. Epub 2013 Oct 1.

Effects of novel human cathepsin S inhibitors on cell migration in human cancer cells.

Author information

1
Department of Life Science, Institute of Biotechnology, National Tsing Hua University , Hsinchu , Taiwan .

Abstract

Elevated cathepsin S (Cat S) level is correlated with higher migration ability in tumor cells. This study investigates the inhibitory effect of novel synthetic α-ketoamide compounds on cathepsin activity and cancer cell migration. The effect of several α-ketoamide compounds on the activity of recombinant cathepsins (Cat S, Cat L and Cat K) was examined. Two highly metastatic cancer cell lines were incubated with three Cat S-specific compounds (6n, 6 w and 6r) to analyze their effect on cellular Cat S activity and cell migration. At a 100 nM concentration, compounds 6n, 6r and 6 w effectively inhibited Cat S activity. Cat S activity and cell migration were significantly reduced in CL1-3 cells after treatment with either 6n or 6 w at 5 μM. Similar results were also obtained when A2058 cells were treated with 6n. These results highlight the therapeutic potential of α-ketoamide compounds, especially 6n and 6 w, to prevent or delay cancer metastasis.

KEYWORDS:

cysteine cathepsin; lung adenocarcinoma; melanoma; α-Ketoamides

PMID:
24083411
DOI:
10.3109/14756366.2013.823957
[Indexed for MEDLINE]

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