Improved quenched fluorescent probe for imaging of cysteine cathepsin activity

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Title:	Improved quenched fluorescent probe for imaging of cysteine cathepsin activity
Author(s):	Verdoes, M.; Bender, K. Oresic; Segal, E.; Linden, W.A. van der; Syed, S.; Withana, N.P.; Sanman, L.E.; Bogyo, M.
Publication year:	2013
Source:	Journal of the American Chemical Society, vol. 135, iss. 39, (2013), pp. 14726-14730
ISSN:	0002-7863
Related links:	http://www.ncbi.nlm.nih.gov/pubmed/23971698
DOI:	https://doi.org/10.1021/ja4056068
Publication type:	Article / Letter to editor
Please use this identifier to cite or link to this item : http://hdl.handle.net/2066/125955
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Subject:	NCMLS 2: Immune Regulation
Organization:	Tumorimmunology
Journal title:	Journal of the American Chemical Society
Volume:	vol. 135
Issue:	iss. 39
Page start:	p. 14726
Page end:	p. 14730
Abstract:	The cysteine cathepsins are a family of proteases that play important roles in both normal cellular physiology and many human diseases. In cancer, the activity of many of the cysteine cathepsins is upregulated and can be exploited for tumor imaging. Here we present the design and synthesis of a new class of quenched fluorescent activity-based probes (qABPs) containing a phenoxymethyl ketone (PMK) electrophile. These reagents show enhanced in vivo properties and broad reactivity resulting in dramatically improved labeling and tumor imaging properties compared to those of previously reported ABPs.