α Vβ 3 Integrins are a widely recognized target for in vivo molecular imaging of pathological conditions such as inflammation, cancer and rheumatoid arthritis. We have evaluated the sensitivity of a new, near-infrared fluorescence (NIRF), RGD cyclic probe (DA364) in noninvasive detection of α Vβ 3 integrin-overexpressing tumors. DA364's binding affinity for α Vβ 3 integrin was first evaluated in vitro. Human α Vβ 3 integrin-positive, U-87 MG glioblastoma cells were then xenografted in nude mice, and DA364 was injected intravenously (i.v.) to evaluate its in vivo distribution, specificity and sensitivity in comparison with a commercially available probe. DA364 bound α Vβ 3 integrin on U-87 MG cells with high affinity and specificity, both in vitro and in vivo. This binding specificity was corroborated by the strong inhibition of its tumor uptake induced by nonfluorescent, cyclic-RGD peptides. Ex vivo analysis showed that DA364 accumulated at the tumor site, whereas very low levels were detected in liver and spleen. In conclusion, DA364 allows sensitive and specific detection of transplantable glioblastoma by NIRF imaging, and is thus a promising candidate for the elaboration of imaging and therapeutic probes for α Vβ 3 integrin-overexpressing tumors.

A new optical imaging probe targeting αVβ3 integrin in glioblastoma xenografts / S. Lanzardo, L. Conti, C. Brioschi, M.P. Bartolomeo, D. Arosio, L. Belvisi, L. Manzoni, A. Maiocchi, F. Maisano, G. Forni. - In: CONTRAST MEDIA & MOLECULAR IMAGING. - ISSN 1555-4309. - 6:6(2011), pp. 449-458. [10.1002/cmmi.444]

A new optical imaging probe targeting αVβ3 integrin in glioblastoma xenografts

L. Belvisi;
2011

Abstract

α Vβ 3 Integrins are a widely recognized target for in vivo molecular imaging of pathological conditions such as inflammation, cancer and rheumatoid arthritis. We have evaluated the sensitivity of a new, near-infrared fluorescence (NIRF), RGD cyclic probe (DA364) in noninvasive detection of α Vβ 3 integrin-overexpressing tumors. DA364's binding affinity for α Vβ 3 integrin was first evaluated in vitro. Human α Vβ 3 integrin-positive, U-87 MG glioblastoma cells were then xenografted in nude mice, and DA364 was injected intravenously (i.v.) to evaluate its in vivo distribution, specificity and sensitivity in comparison with a commercially available probe. DA364 bound α Vβ 3 integrin on U-87 MG cells with high affinity and specificity, both in vitro and in vivo. This binding specificity was corroborated by the strong inhibition of its tumor uptake induced by nonfluorescent, cyclic-RGD peptides. Ex vivo analysis showed that DA364 accumulated at the tumor site, whereas very low levels were detected in liver and spleen. In conclusion, DA364 allows sensitive and specific detection of transplantable glioblastoma by NIRF imaging, and is thus a promising candidate for the elaboration of imaging and therapeutic probes for α Vβ 3 integrin-overexpressing tumors.
Settore CHIM/06 - Chimica Organica
Article (author)
File in questo prodotto:
Non ci sono file associati a questo prodotto.
Pubblicazioni consigliate

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/165559
Citazioni
  • ???jsp.display-item.citation.pmc??? 11
  • Scopus 36
  • ???jsp.display-item.citation.isi??? 37
social impact