title: A desferrioxamine B squaramide ester for the incorporation of zirconium-89 into antibodies.
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.
authors.affiliation: School of Chemistry and Bio21 Molecular Science and Biotechnology Institute, University of Melbourne, Melbourne, Victoria 3010, Australia. pauld@unimelb.edu.au.
authors.forename: Stacey E
authors.initials: SE
authors.lastname: Rudd
authors.affiliation: Research Division, Peter MacCallum Cancer Centre, 305 Grattan St, Melbourne 3000, Victoria, Australia.
authors.forename: Peter
authors.initials: P
authors.lastname: Roselt
authors.affiliation: Research Division, Peter MacCallum Cancer Centre, 305 Grattan St, Melbourne 3000, Victoria, Australia and The Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC, Australia. Rod.Hicks@petermac.org.
authors.forename: Carleen
authors.initials: C
authors.lastname: Cullinane
authors.affiliation: The Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC, Australia. Rod.Hicks@petermac.org and Centre for Cancer Imaging, Peter MacCallum Cancer Centre, 305 Grattan St, Melbourne 3000, Victoria, Australia.
authors.forename: Rodney J
authors.initials: RJ
authors.lastname: Hicks
authors.affiliation: School of Chemistry and Bio21 Molecular Science and Biotechnology Institute, University of Melbourne, Melbourne, Victoria 3010, Australia. pauld@unimelb.edu.au.
authors.forename: Paul S
authors.initials: PS
authors.lastname: Donnelly
mesh_terms: D000818:Animals; D061067:Antibodies, Monoclonal, Humanized / Q000737:chemistry* / Q000276:immunology; D001943:Breast Neoplasms / Q000175:diagnosis / Q000000981:diagnostic imaging; D045744:Cell Line, Tumor; D003676:Deferoxamine / Q000737:chemistry*; D004195:Disease Models, Animal; D005260:Female; D006801:Humans; D007553:Isotope Labeling; D051379:Mice; D049268:Positron-Emission Tomography; D011868:Radioisotopes / Q000737:chemistry; D018719:Erb-b2 Receptor Tyrosine Kinases / Q000276:immunology / Q000378:metabolism; D014183:Transplantation, Heterologous; D000068878:Trastuzumab / Q000737:chemistry* / Q000276:immunology; D015040:Zirconium / Q000737:chemistry
chemical_list: D061067:Antibodies, Monoclonal, Humanized; D003676:Deferoxamine; D011868:Radioisotopes; D018719:Erb-b2 Receptor Tyrosine Kinases; D000068878:Trastuzumab; D015040:Zirconium; C000615502:Zirconium-89