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Tissue-Penetrating Delivery of Compounds and Nanoparticles into Tumors
Open accessAbstract
SUMMARY Poor penetration of drugs into tumors is a major obstacle in tumor treatment. We describe a strategy for peptide-mediated delivery of compounds deep into the tumor parenchyma that employs a tumor homing peptide, iRGD (CRGDK/RGPD/EC). Intravenously injected compounds coupled to iRGD bound to tumor vessels and spread into the extravascular tumor parenchyma, whereas conventional RGD peptides only delivered the cargo to the blood vessels. iRGD homes to tumors through a 3-step process: The RGD motif mediates binding to αv integrins on tumor endothelium, a proteolytic cleavage then exposes a binding motif for neuropilin-1, which mediates penetration into tissue and cells. Conjugation to iRGD significantly improved the sensitivity of tumor imaging agents and enhanced the activity of an anti-tumor drug.
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Metadata
- Authors
- Sugahara, K. N., Teesalu, T., Karmali, P. P., Kotamraju, V. R., Agemy, L., Girard, O. M., Hanahan, D., Mattrey, R. F., & Ruoslahti, E.
- Venue
- Cancer Cell
- Publisher
- Elsevier BV
- Published
- 2009-12
- Volume
- 16
- Issue
- 6
- Pages
- 510-520
- ISSN
- 1535-6108 (ISSN-L)
- OpenAlex
- W2163326536
- Cited by
- 1,136
- References
- 5
- FWCI
- 18.73
- Type
- journal article
- Language
- en
- Open access
- bronze
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