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Cyclic arginine-glycine-aspartic acid tripeptide (cRGD) is a cyclic peptide motif that specifically binds to integrin receptors, most notably integrin alpha-V beta-3 (αvβ3). This integrin is highly expressed on the surface of various tumor cells and the endothelial cells of tumor-associated blood vessels, making cRGD an effective targeting ligand for cancer therapy and imaging. By mimicking the natural binding sequence found in extracellular matrix proteins like fibronectin and vitronectin, cRGD can be conjugated to various therapeutic payloads—including small molecules, nanoparticles, oncolytic viruses, and photosensitizers—to enhance their selective delivery to tumor tissues. This targeted approach aims to increase local drug concentration while reducing systemic toxicity.
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