Molecules, Vol. 25, Pages 2315: 89Zr-Labeled AR20.5: A MUC1-Targeting ImmunoPET Probe
Molecules, Vol. 25, Pages 2315: 89Zr-Labeled AR20.5: A MUC1-Targeting ImmunoPET Probe
Molecules doi: 10.3390/molecules25102315
Authors:
Kimberly Fung
Delphine Vivier
Outi Keinänen
Elaheh Khozeimeh Sarbisheh
Eric W. Price
Brian M. Zeglis
High expression levels of the tumor-associated antigen MUC1 have been correlated with tumor aggressiveness, poor response to therapy, and poor survival in several tumor types, including breast, pancreatic, and epithelial ovarian cancer. Herein, we report the synthesis, characterization, and in vivo evaluation of a novel radioimmunoconjugate for the immuno-positron emission tomography (immunoPET) imaging of MUC1 expression based on the AR20.5 antibody. To this end, we modified AR20.5 with the chelator desferrioxamine (DFO) and labeled it with the positron-emitting radiometal zirconium-89 (t1/2 ~3.3 d) to produce [89Zr]Zr-DFO-AR20.5. In subsequent in vivo experiments in athymic nude mice bearing subcutaneous MUC1-expressing ovarian cancer xenografts, [89Zr]Zr-DFO-AR20.5 clearly delineated tumor tissue, producing a tumoral activity concentration of 19.1 ± 6.4 percent injected dose per gram (%ID/g) at 120 h post-injection and a tumor-to-muscle activity concentration ratio of 42.4 ± 10.6 at the same time point. Additional PET imaging experiments in mice bearing orthotopic MUC1-expressing ovarian cancer xenografts likewise demonstrated that [89Zr]Zr-DFO-AR20.5 enables the visualization of tumor tissue...
Source: Molecules - Category: Chemistry Authors: Kimberly Fung Delphine Vivier Outi Kein änen Elaheh Khozeimeh Sarbisheh Eric W. Price Brian M. Zeglis Tags: Article Source Type: research
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