title: Improved quenched fluorescent probe for imaging of cysteine cathepsin activity.
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.
authors: Departments of †Pathology, ‡Cancer Biology Program, and §Microbiology and Immunology, Stanford School of Medicine , 300 Pasteur Drive, Stanford, California 94305-5324, United States.
authors: Martijn
authors: M
authors: Verdoes
authors: Kristina
authors: K
authors: Oresic Bender
authors: Ehud
authors: E
authors: Segal
authors: Wouter A
authors: WA
authors: van der Linden
authors: Salahuddin
authors: S
authors: Syed
authors: Nimali P
authors: NP
authors: Withana
authors: Laura E
authors: LE
authors: Sanman
authors: Matthew
authors: M
authors: Bogyo
mesh_terms: D000818:Animals; D001940:Breast / Q000201:enzymology / Q000473:pathology*; D001943:Breast Neoplasms / Q000175:diagnosis* / Q000201:enzymology* / Q000473:pathology; D002460:Cell Line; D002478:Cells, Cultured; D003545:Cysteine / Q000378:metabolism; D057056:Cysteine Proteases / Q000032:analysis* / Q000378:metabolism; D005260:Female; D005456:Fluorescent Dyes / Q000138:chemical synthesis / Q000737:chemistry*; D006801:Humans; D007659:Ketones / Q000138:chemical synthesis / Q000737:chemistry; D051379:Mice; D061848:Optical Imaging / Q000379:methods
chemical_list: D005456:Fluorescent Dyes; D007659:Ketones; D057056:Cysteine Proteases; D003545:Cysteine
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