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Optical imaging with a novel cathepsin-activatable probe for enhanced detection of colorectal cancer.


ABSTRACT: We evaluated a cysteine cathepsin-activatable optical imaging probe (LUM015) with improved kinetics relative to larger macromolecules for detection and characterization of colorectal cancer (CRC), and thereby assessed its potential use in fluorescence-guided colonoscopy. We showed that LUM015 is stable in plasma. In-vitro studies demonstrated selectivity of LUM015 for targeting cathepsins; there was robust increase in emitted fluorescence signal from the cathepsin overexpressing HT-29 CRC cells within 1-5 minutes after incubation with LUM015 compared to the cells incubated with combination of LUM015 and a pan-protease inhibitor (as negative control). Biodistribution, differential accumulation of the probe in the tumor and tumor-to-background fluorescence signal ratio of LUM015 were compare

SUBMITTER: Esfahani SA 

PROVIDER: S-EPMC6872479 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature