IRGCs |
IRH |
Tyr-Pro-Val-Glu-Pro |
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[internalizing-RGD] This peptide with the sequence CRGDKGPDC has been identified as a tumor-penetrating peptide by virtue of its ability to bind to, and to be internalized by, cultured PPC1 human prostate cancer cell (Sugahara et al, 2009). Intravenously injected compounds coupled to iRGD bind to tumor vessels and spread into the extravascular tumor parenchyma, whereas conventional RGD peptides only deliver the cargo to the blood vessels. iRGD homes to tumors by binding initially to integrin-alpha-V / integrin-beta-5 and integrin-alpha-5 / integrin-beta-1. Proteolytic cleavage then exposes a cryptic C-end Rule peptide
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