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Cyclic RGD peptide-labeled upconversion nanophosphors for tumor cell-targeted imaging
Authors:Tamotsu Zako  Hiroyasu Nagata  Naofumi Terada  Masafumi Sakono  Hiroshi Ueda  Mizuo Maeda
Institution:a Bioengineering Laboratory, RIKEN Institute, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan
b Department of Materials Science and Technology, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan
c Department of Biotechnology and Life Science, Tokyo University of Agriculture and Technology, 2-24-16 Naka-cho, Koganei, Tokyo 184-8588, Japan
d Department of Chemistry and Biotechnology, School of Engineering, The University of Tokyo, 7-3-1, Hongo, Bunkyo, Tokyo 113-8656, Japan
Abstract:One of the great challenges of oncology is to improve methods for early tumor detection. Thus tumor cell-targeted optical imaging has been intensively studied. Bioimaging with upconversion (UC) phosphors (UCPs) is of considerable interest due to a variety of possible applications taking advantage of infrared-to-visible luminescence. Here we report for the first time tumor cell-targeted UC imaging using UCPs modified with cyclic RGD peptide (RGD-Y2O3). Cyclic RGD peptide binds specifically to integrin αvβ3 which is highly expressed in a tumor cell surface of certain cancer types but not in normal tissues. Since UC emission from RGD-Y2O3 was observed for U87MG cancer cell (high integrin αvβ3 expression), but not for MCF-7 cancer cell (low integrin αvβ3 expression), this UC imaging is considered to be integrin αvβ3 specific. The non-invasive imaging of integrin αvβ3 expression using UCP-based probes will have great potential in cancer imaging in general in living subjects.
Keywords:Upconversion  Bioimaging  Nanoparticles  Tumor imaging  Cancer  PEG modification  Integrin αvβ3  RGD peptide
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