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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.

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.

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