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Molecules. 2014 Aug 5;19(8):11600-12. doi: 10.3390/molecules190811600.

68Ga-labeled cyclic NGR peptide for microPET imaging of CD13 receptor expression.

Author information

1
Department of Nuclear Medicine, Xijing Hospital, The Fourth Military Medical University, Xi'an 710032, China.
2
Department of Nuclear Medicine, Lanzhou General Hospital of Lanzhou Military Area Command, Lanzhou 730050, China.
3
Molecular Imaging Center, Department of Radiology, Keck School of Medicine, University of Southern California, Los Angeles, CA 90033, USA. chenkai@usc.edu.
4
Department of Nuclear Medicine, Xijing Hospital, The Fourth Military Medical University, Xi'an 710032, China. wangjing@fmmu.edu.cn.

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 (68)Ga (t1/2 = 67.7 min). The resulting (68)Ga-NOTA-G3-NGR peptide was subject to in vitro and in vivo characterization. The microPET imaging results revealed that the (68)Ga-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 (68)Ga-NOTA-G3-NGR peptide has potential in the diagnosis of CD13-targeted tumor angiogenesis.

PMID:
25100253
DOI:
10.3390/molecules190811600
[Indexed for MEDLINE]
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