AJNMMI Copyright © 2011-present, All rights reserved. Published by e-Century Publishing Corporation, Madison, WI 53711, USA
Am J Nucl Med Mol Imaging 2011;1(1):36-46.

Review article
Development of NGR peptide-based agents for tumor imaging

Rongsheng E Wang, Youhong Niu, Haifan Wu, Mohamad Nassir Amin, Jianfeng Cai


Department of Chemistry, Washington University in St. Louis, St. Louis, MO 63130, USA; Department of Chemistry, University of
South Florida, 4202 E. Fowler Ave, Tampa, FL, 33620, USA.

Received June 10, 2011; accepted June 22, 2011; Epub June 23, 2011; Published August 1, 2011

Abstract: Molecular imaging allows direct visualization of targets and characterization of cellular pathways, as long as a high
signal/background ratio can be achieved, which requires a sufficient amount of probes to accumulate in the imaging region. The
Asn-Gly-Arg (NGR) tripeptide selected by phage display can specifically target tumor vasculature.  Recognizing the aminopeptidase
N (APN or CD13) receptor on the membrane of tumor cells, the peptide can be further internalized into cytoplasma by the endosomal
pathway.  Hence NGR can serve as an ideal candidate for tumor imaging, once it is conjugated with fluorescent or radiolabeled
imaging probes.  Herein, we highlighted some recent developments of NGR peptide based imaging of tumors.  Although still in the
preliminary stage, some NGR probes have shown potential as promising agents in future clinical applications.  (ajnmmi1106003).

Keywords: Asparagine-glycine-arginine (NGR), arginine-glycine-aspartic acid (RGD), isoaspartate-glycine-arginine (isoDGR),
cancer, imaging, tumor angiogenesis, vasculature, aminopeptidase N (APN/CD13)

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Address all correspondence to:
Jianfeng Cai, PhD
Department of Chemistry
University of South Florida
4202 E. Fowler Ave
Tampa, FL, 33620, USA.
E-mail: Jianfengcai@usf.edu