(89)Zr-labeled AR20.5: A MUC1-targeting ImmunoPET probe Journal Article


Authors: Fung, K.; Vivier, D.; Keinänen, O.; Sarbisheh, E. K.; Price, E. W.; Zeglis, B. M.
Article Title: (89)Zr-labeled AR20.5: A MUC1-targeting ImmunoPET probe
Abstract: 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—including metastatic lesions—with promising tumor-to-background contrast. © 2020 by the authors.
Keywords: positron emission tomography; mucin 1; pet; zirconium-89; muc1; ar20.5
Journal Title: Molecules
Volume: 25
Issue: 10
ISSN: 1420-3049
Publisher: MDPI  
Date Published: 2020-05-01
Start Page: 2315
Language: English
DOI: 10.3390/molecules25102315
PUBMED: 32429033
PROVIDER: scopus
DOI/URL:
Notes: Article -- Export Date: 1 June 2020 -- Source: Scopus
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  1. Brian Zeglis
    78 Zeglis