Matrix metalloproteinase-14 (MT1-MMP or MMP-14) is an internalized cell-surface protease implicated in various metastatic cancers.  The ability to detect MMP-14 tumor cells in vivo would be useful in diagnosing early stage cancers.  Our design of small-molecule probes for in vitro detection of MMP-14 positive cells includes a MMP-14 inhibitor linked to a fluorescent dye.  Analogs of known MMP-14 inhibitors such as hydroxamate-containing sulfonamides as well as a new class of phosphoramidates are currently under investigation.  Progress toward the development of these probes as well as results for the inhibitory potency of fluorescent MMP-14 inhibitors and in vitro cell labeling as detected by confocal microscopy will be presented.

Design, synthesis, and biological evaluation of MMP-14 inhibitors

239th National Meeting (2010)

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