Theranostics 2011; 1:102-126. doi:10.7150/thno/v01p0102 This volume


Integrin Targeting for Tumor Optical Imaging

Yunpeng Ye, Xiaoyuan Chen

National Institute of Biomedical Imaging and Bioengineering (NIBIB), National Institute of Health (NIH), Bethesda, MD

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Ye Y, Chen X. Integrin Targeting for Tumor Optical Imaging. Theranostics 2011; 1:102-126. doi:10.7150/thno/v01p0102. Available from

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Optical imaging has emerged as a powerful modality for studying molecular recognitions and molecular imaging in a noninvasive, sensitive, and real-time way. Some advantages of optical imaging include cost-effectiveness, convenience, and non-ionization safety as well as complementation with other imaging modalities such as positron emission tomography (PET), single-photon emission computed tomography (SPECT), and magnetic resonance imaging (MRI). Over the past decade, considerable advances have been made in tumor optical imaging by targeting integrin receptors in preclinical studies. This review has emphasized the construction and evaluation of diverse integrin targeting agents for optical imaging of tumors in mouse models. They mainly include some near-infrared fluorescent dye-RGD peptide conjugates, their multivalent analogs, and nanoparticle conjugates for targeting integrin αvβ3. Some compounds targeting other integrin subtypes such as α4β1 and α3 for tumor optical imaging have also been included. Both in vitro and in vivo studies have revealed some promising integrin-targeting optical agents which have further enhanced our understanding of integrin expression and targeting in cancer biology as well as related anticancer drug discovery. Especially, some integrin-targeted multifunctional optical agents including nanoparticle-based optical agents can multiplex optical imaging with other imaging modalities and targeted therapy, serving as an attractive type of theranostics for simultaneous imaging and targeted therapy. Continued efforts to discover and develop novel, innovative integrin-based optical agents with improved targeting specificity and imaging sensitivity hold great promises for improving cancer early detection, diagnosis, and targeted therapy in clinic.

Keywords: optical imaging, near-infrared fluorescence, multivalent RGD peptides, multifunctional probes, nanoparticle-based optical agents.