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Nat Biotechnol. 1997 Jun;15(6):542-6.

Alpha v integrins as receptors for tumor targeting by circulating ligands.

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La Jolla Cancer Research Center, Burnham Institute, La Jolla, CA, USA. (RP); (ER)


Phage displaying an Arg-Gly-Asp (RGD)-containing peptide with a high affinity for alpha v integrins homed to tumors when injected intravenously into tumor-bearing mice. A substantially higher amount of alpha v-directed RGD phage than control phage was recovered from malignant melanomas and breast carcinoma. Antibodies detected the alpha v-directed RGD phage in tumor blood vessels, but not in several normal tissues. These results show that the alpha v integrins present in tumor blood vessels can bind circulating ligands and that RGD peptides selective for these integrins may be suitable tools in tumor targeting for diagnostic and therapeutic purposes.

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