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Molecules 2014, 19(8), 11600-11612;

68Ga-Labeled Cyclic NGR Peptide for MicroPET Imaging of CD13 Receptor Expression

Department of Nuclear Medicine, Xijing Hospital, The Fourth Military Medical University, Xi'an 710032, China
Department of Nuclear Medicine, General Hospital of Jinan Military Area Command, Jinan 250031, China
Department of Nuclear Medicine, Lanzhou General Hospital of Lanzhou Military Area Command, Lanzhou 730050, China
Molecular Imaging Center, Department of Radiology, Keck School of Medicine, University of Southern California, Los Angeles, CA 90033, USA
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Received: 26 May 2014 / Revised: 14 July 2014 / Accepted: 25 July 2014 / Published: 5 August 2014
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Peptides containing the asparagines-glycine-arginine (NGR) motif have been identified as specific ligands binding to CD13/aminopeptidase N (APN) receptor, a tumor neovascular biomarker. In this study, we synthesized a novel NGR-containing peptide (NOTA-G3-NGR), and labeled NOTA-G3-NGR with 68Ga (t1/2 = 67.7 min). The resulting 68Ga-NOTA-G3-NGR peptide was subject to in vitro and in vivo characterization. The microPET imaging results revealed that the 68Ga-NOTA-G3-NGR peptide exhibits rapid and specific tumor uptake, and high tumor-to-background contrast in a subcutaneous HT-1080 fibrosarcoma mouse model. We concluded that the 68Ga-NOTA-G3-NGR peptide has potential in the diagnosis of CD13-targeted tumor angiogenesis. View Full-Text
Keywords: microPET imaging; NGR peptide; CD13; tumor angiogenesis; 68Ga labeling microPET imaging; NGR peptide; CD13; tumor angiogenesis; 68Ga labeling

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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Shao, Y.; Liang, W.; Kang, F.; Yang, W.; Ma, X.; Li, G.; Zong, S.; Chen, K.; Wang, J. 68Ga-Labeled Cyclic NGR Peptide for MicroPET Imaging of CD13 Receptor Expression. Molecules 2014, 19, 11600-11612.

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