2-Nitroimidazole-tricarbocyanine conjugate as a near-infrared fluorescent probe for in vivo imaging of tumor hypoxia.

Autor: Okuda K; Laboratory of Pharmaceutical and Medicinal Chemistry, Gifu Pharmaceutical University, Gifu 501-1196, Japan., Okabe Y, Kadonosono T, Ueno T, Youssif BG, Kizaka-Kondoh S, Nagasawa H
Jazyk: angličtina
Zdroj: Bioconjugate chemistry [Bioconjug Chem] 2012 Mar 21; Vol. 23 (3), pp. 324-9. Date of Electronic Publication: 2012 Feb 22.
DOI: 10.1021/bc2004704
Abstrakt: We developed a novel near-infrared (NIR) fluorescent probe, GPU-167, for in vivo imaging of tumor hypoxia. GPU-167 comprises a tricarbocyanine dye as an NIR fluorophore and two 2-nitroimidazole moieties as exogenous hypoxia markers that undergo bioreductive activation and then selective entrapment in hypoxic cells. After treatment with GPU-167, tumor cells contained significantly higher levels of fluorescence in hypoxia than in normoxia. In vivo fluorescence imaging specifically detected GPU-167 in tumors 24 h after administration. Ex vivo analysis revealed that fluorescence showed a strong correlation with hypoxia inducible factor (HIF)-1 active hypoxic regions. These data suggest that GPU-167 is a promising in vivo optical imaging probe for tumor hypoxia.
Databáze: MEDLINE