Journal article
Non-invasive imaging of cysteine cathepsin activity in solid tumors using a 64Cu-labeled activity-based probe
G Ren, G Blum, M Verdoes, H Liu, S Syed, LE Edgington, O Gheysens, Z Miao, H Jiang, SS Gambhir, M Bogyo, Z Cheng
Plos One | PUBLIC LIBRARY SCIENCE | Published : 2011
Open access
Abstract
The papain family of cysteine cathepsins are actively involved in multiple stages of tumorigenesis. Because elevated cathepsin activity can be found in many types of human cancers, they are promising biomarkers that can be used to target radiological contrast agents for tumor detection. However, currently there are no radiological imaging agents available for these important molecular targets. We report here the development of positron emission tomography (PET) radionuclide-labeled probes that target the cysteine cathepsins by formation of an enzyme activity-dependent bond with the active site cysteine. These probes contain an acyloxymethyl ketone (AOMK) functional group that irreversibly la..
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Awarded by National Cancer Institute
Funding Acknowledgements
This work was supported, in part, by National Institutes of Health (NIH) National Technology Centers for Networks and Pathways grant U54 RR020843 (MB), NIH grant R01 EB005011 (MB), Susan G. Komen for the Cure grant PDF0504576 (GB), National Cancer Institute (NCI) Small Animal Imaging Resource Program (SAIRP) grant R24 CA93862, and NCI In Vivo Cellular Molecular Imaging Center (ICMIC) grant P50 CA114747 (SSG). The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.