Issue 80, 2016
From the journal:

Chemical Communications

A desferrioxamine B squaramide ester for the incorporation of zirconium-89 into antibodies†

Stacey E. Rudd,a   Peter Roselt,b   Carleen Cullinane,bc   Rodney J. Hicks*cd  and  Paul S. Donnelly*a  

* Corresponding authors

a School of Chemistry and Bio21 Molecular Science and Biotechnology Institute, University of Melbourne, Melbourne, Victoria, Australia
E-mail: pauld@unimelb.edu.au

b Research Division, Peter MacCallum Cancer Centre, 305 Grattan St, Melbourne 3000, Victoria, Australia

c The Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC, Australia
E-mail: Rod.Hicks@petermac.org

d Centre for Cancer Imaging, Peter MacCallum Cancer Centre, 305 Grattan St, Melbourne 3000, Victoria, Australia

Abstract

A squaramide ester derivative of desferrioxamine B (H3DFO) that is compatible with aqueous solvents and does not induce antibody aggregation is used to attach the siderophore to the antibody trastuzumab. The new conjugates were radiolabeled with zirconium-89 to give complexes that are more resistant to ligand exchange when compared to currently used H3DFO derivatives and result in high quality positron emission tomography images in mouse models of HER2 positive breast cancer.

Graphical abstract: A desferrioxamine B squaramide ester for the incorporation of zirconium-89 into antibodies

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Article information

DOI
https://doi.org/10.1039/C6CC05961A
Article type
Communication
Submitted
20 Jul 2016
Accepted
19 Aug 2016
First published
19 Aug 2016

Chem. Commun., 2016,52, 11889-11892

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A desferrioxamine B squaramide ester for the incorporation of zirconium-89 into antibodies

S. E. Rudd, P. Roselt, C. Cullinane, R. J. Hicks and P. S. Donnelly, Chem. Commun., 2016, 52, 11889 DOI: 10.1039/C6CC05961A

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