Development of near-infrared fluorophore (NIRF)-labeled activity-based probes for in vivo imaging of legumain.

ABSTRACT: Asparaginyl endopeptidase, or legumain, is a lysosomal cysteine protease that was originally identified in plants and later found to be involved in antigen presentation in higher eukaryotes. Legumain is also up-regulated in a number of human cancers, and recent studies suggest that it may play important functional roles in the process of tumorigenesis. However, detailed functional studies in relevant animal models of human disease have been hindered by the lack of suitably selective small molecule inhibitors and imaging reagents. Here we present the design, optimization, and in vivo application of fluorescently labeled activity-based probes (ABPs) for legumain. We demonstrate that optimized aza-peptidyl Asn epoxides are highly selective and potent inhibitors that can be readily converted i

SUBMITTER: Lee J 

PROVIDER: S-EPMC3222276 | biostudies-literature | 2010 Feb

REPOSITORIES: biostudies-literature