Background:

NGR peptide Trifluoroacetate containing the asparagine-glycine-arginine (NGR) motif is recognized by CD13/aminopeptidase N (APN) receptor isoforms that are selectively overexpressed in tumor neovasculature.

NGR peptide can selectively bind to APN/CD13 either immune-captured or expressed on the surface of cells, the receptor of the tumor-homing NGR peptide was suspected to be APN/CD13. The NGR peptide is reported to have the greatest tumor selectivity. An anti-cancer drug Doxorubicin (DOX) coupled to an NGR peptide displays enhanced anti-tumor effects with even lower toxicity than the free drug itself[2].

NGR peptide imaging in vivo not only provides more insight into NGR’s targeting process, including bio-distribution and pharmacokinetics, but also reveals angiogenic activities related to tumor progression and malignancy[2].

参考文献:
[1]. Enyedi KN, et al. NGR-peptide-drug conjugates with dual targeting properties. NGR-peptide-drug conjugates with dual targeting properties.
[2]. Wang RE, et al. Development of NGR peptide-based agents for tumor imaging. Am J Nucl Med Mol Imaging. 2011;1(1):36-46.