Publication year
2013Source
Journal of the American Chemical Society, 135, 1, (2013), pp. 174-82ISSN
Publication type
Article / Letter to editor
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Organization
Tumorimmunology
Journal title
Journal of the American Chemical Society
Volume
vol. 135
Issue
iss. 1
Page start
p. 174
Page end
p. 82
Subject
NCMLS 2: Immune RegulationAbstract
Legumain is a lysosomal cysteine protease whose biological function remains poorly defined. Legumain activity is up-regulated in most human cancers and inflammatory diseases most likely as the result of high expression in populations of activated macrophages. Within the tumor microenvironment, legumain activity is thought to promote tumorigenesis. To obtain a greater understanding of the role of legumain activity during cancer progression and inflammation, we developed an activity-based probe that becomes fluorescent only upon binding active legumain. This probe is highly selective for legumain, even in the context of whole cells and tissues, and is also a more effective label of legumain than previously reported probes. Here we present the synthesis and application of our probe to the analysis of legumain activity in primary macrophages and in two mouse models of cancer. We find that legumain activity is highly correlated with macrophage activation and furthermore that it is an ideal marker for primary tumor inflammation and early stage metastatic lesions.
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- Academic publications [245050]
- Faculty of Medical Sciences [93209]
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