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Molecules 2014, 19(8), 11600-11612; doi:10.3390/molecules190811600

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

1
Department of Nuclear Medicine, Xijing Hospital, The Fourth Military Medical University, Xi'an 710032, China
2
Department of Nuclear Medicine, General Hospital of Jinan Military Area Command, Jinan 250031, China
3
Department of Nuclear Medicine, Lanzhou General Hospital of Lanzhou Military Area Command, Lanzhou 730050, China
4
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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Abstract

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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MDPI and ACS Style

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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