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• W2055144800 abstract "The development of molecular probes based on novel engineered protein constructs is under active investigation due to the great potential of this generalizable strategy for imaging a variety of tumor targets. In this report, human epidermal growth factor receptor type 2 (HER2)-binding Affibody molecules were radiolabeled with 64Cu and their imaging ability was further evaluated in tumor mice models to understand the promise and limitations of such probes. The anti-HER2 Affibody molecules in monomeric (ZHER2:477) and dimeric [(ZHER2:477)2] forms were site specifically modified with the maleimide-functionalized chelator, 1,4,7,10-tetraazacyclododecane-1,4,7-tris(acetic acid)-10-acetate mono (N-ethylmaleimide amide) (Mal-DOTA). The resulting DOTA–Affibody conjugates were radiolabeled with 64Cu and evaluated in nude mice bearing subcutaneous SKOV3 tumors. Biodistribution experiments showed that tumor uptake values of 64Cu-DOTA-ZHER2:477 and 64Cu-DOTA-(ZHER2:477)2 were 6.12 ± 1.44% and 1.46 ± 0.50% ID/g, respectively, in nude mice (n = 3 each) at 4 h postinjection. Moreover, 64Cu-labeled monomer exhibited significantly higher tumor/blood ratio than that of radiolabeled dimeric counterpart at all time points examined in this study. MicroPET imaging of 64Cu-DOTA-ZHER2:477 in SKOV3 tumor mice clearly showed good and specific tumor localization. This study demonstrates that 64Cu-labeled ZHER2:477 is a promising targeted molecular probe for imaging HER2 receptor expression in living mice. Further work is needed to improve the excretion properties, hence dosimetry and imaging efficacy, of the radiometal-based probe." @default.
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• W2055144800 date "2009-09-25" @default.
• W2055144800 modified "2023-09-30" @default.
• W2055144800 title "64Cu-Labeled Affibody Molecules for Imaging of HER2 Expressing Tumors" @default.
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• W2055144800 doi "https://doi.org/10.1007/s11307-009-0256-6" @default.
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