Abstract
Cathepsin B (CTSB) is a lysosomal protease, and several human cancers are reported highly expressing CTSB. Many optical methods have been developed for CTSB detection but not a bioluminescence (BL) probe. Herein, a CTSB-specific bioluminescence probe Val-Cit-AL was rationally designed for selectively sensing CTSB activity in vitro with a 67-fold "Turn-On" of BL intensity and an excellent limit of detection. Inhibitory experiments indicated that Val-Cit-AL is capable of sensing CTSB activity in living cells and tumors. We anticipate that Val-Cit-AL might be applied to diagnose CTSB-related diseases in rodent models or evaluate CTSB roles in more biological processes in the near future.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Biomarkers, Tumor / antagonists & inhibitors
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Biomarkers, Tumor / genetics*
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Biomarkers, Tumor / metabolism
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Breast Neoplasms / diagnostic imaging*
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Breast Neoplasms / genetics
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Breast Neoplasms / metabolism
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Breast Neoplasms / pathology
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Cathepsin B / antagonists & inhibitors
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Cathepsin B / genetics*
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Cathepsin B / metabolism
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Cell Line, Tumor
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Diagnostic Imaging / methods*
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Dipeptides / pharmacology
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Female
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Gene Expression
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Heterografts
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Humans
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Luminescent Measurements
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Lysosomes / drug effects
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Lysosomes / enzymology
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Mice
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Mice, Inbred BALB C
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Mice, Nude
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Molecular Probes / chemical synthesis
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Molecular Probes / pharmacokinetics*
Substances
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Biomarkers, Tumor
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CA 074 methyl ester
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Dipeptides
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Molecular Probes
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CTSB protein, human
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Cathepsin B