Tissue-penetrating delivery of compounds and nanoparticles into tumors.
Cancer Cell
; 16(6): 510-20, 2009 Dec 08.
Article
em En
| MEDLINE
| ID: mdl-19962669
ABSTRACT
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 uses 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 three-step process the RGD motif mediates binding to alphav integrins on tumor endothelium and 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 antitumor drug.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Nanopartículas
/
Neoplasias
/
Neoplasias Experimentais
/
Antineoplásicos
Limite:
Animals
Idioma:
En
Ano de publicação:
2009
Tipo de documento:
Article