AJNMMI Copyright © 2011-present, All rights reserved. Published by e-Century Publishing Corporation, Madison, WI 53711, USA
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Am J Nucl Med Mol Imaging 2011;1(1):3-17.
Review article
Design of “smart” probes for optical imaging of apoptosis
Xinglu Huang, Seulki Lee, Xiaoyuan Chen
Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineering (NIBIB) ,
Bethesda, MD, USA.
Received June 6, 2011; accepted June 18, 2011; Epub June 22, 2011; Published August 1, 2011
Abstract: Apoptosis is a mode of programmed cell death in multicellular organisms and plays a central role in controlling embryonic
development, growth and differentiation and monitoring the induction of tumor cell death through anticancer therapy. Since the most
effective chemotherapeutics rely on apoptosis, imaging apoptotic processes can be an invaluable tool to monitor therapeutic
intervention and discover new drugs modulating apoptosis. The most attractive target for developing specific apoptosis imaging
probes is caspases, crucial mediators of apoptosis. Up to now, various optical imaging strategies for apoptosis have been
developed as an easy and economical modality. However, current optical applications are limited by poor sensitivity and specificity. A
subset of molecular imaging contrast agents known as “activatable” or “smart” molecular probes allow for very high signal-to-
background ratios compared with conventional targeted contrast agents and open up the possibility of imaging intracellular targets.
In this review, we will discuss the unique design strategies and applications of activatable probes recently developed for
fluorescence and bioluminescence imaging of caspase activity. (ajnmmi1106002).
Keywords: Activatable probes, apoptosis, bioluminescence, caspases, optical imaging
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Address all correspondence to:
Xiaoyuan Chen, PhD
National Institute of Biomedical Imaging and Bioengineering (NIBIB)
National Institutes of Health (NIH), Bethesda, Maryland 20892, USA.
E-mail; Shawn.Chen@nih.gov and Seulki.Lee@nih.gov