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Methods to Enhance the Metabolic Stability of Peptide-Based PET Radiopharmaceuticals

89Zr-Labeled AR20.5: A MUC1-Targeting ImmunoPET Probe

Department of Chemistry, Hunter College, City University of New York, New York, NY 10021, USA
Ph.D. Program in Chemistry, The Graduate Center of the City University of New York, New York, NY 10016, USA
Department of Radiology, Memorial Sloan Kettering Cancer Center, New York, NY 10021, USA
Department of Chemistry, University of Saskatchewan, Saskatoon, SK S7N 5B5, Canada
Department of Radiology, Weill Cornell Medical College, New York, NY 10021, USA
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editors: João Paulo C. Tomé, Jason S. Lewis and Patricia Pereira
Molecules 2020, 25(10), 2315;
Received: 7 April 2020 / Revised: 30 April 2020 / Accepted: 10 May 2020 / Published: 15 May 2020
(This article belongs to the Special Issue Immunoconjugates for Cancer Imaging and Therapy)
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. View Full-Text
Keywords: mucin 1; MUC1; positron emission tomography; PET; AR20.5; zirconium-89 mucin 1; MUC1; positron emission tomography; PET; AR20.5; zirconium-89
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MDPI and ACS Style

Fung, K.; Vivier, D.; Keinänen, O.; Sarbisheh, E.K.; Price, E.W.; Zeglis, B.M. 89Zr-Labeled AR20.5: A MUC1-Targeting ImmunoPET Probe. Molecules 2020, 25, 2315.

AMA Style

Fung K, Vivier D, Keinänen O, Sarbisheh EK, Price EW, Zeglis BM. 89Zr-Labeled AR20.5: A MUC1-Targeting ImmunoPET Probe. Molecules. 2020; 25(10):2315.

Chicago/Turabian Style

Fung, Kimberly, Delphine Vivier, Outi Keinänen, Elaheh K. Sarbisheh, Eric W. Price, and Brian M. Zeglis 2020. "89Zr-Labeled AR20.5: A MUC1-Targeting ImmunoPET Probe" Molecules 25, no. 10: 2315.

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