Investigation of novel bis- and tris-tetraazamacrocycles for use in the copper-64 (Cu-64) radiolabeling of antibodies with potential to increase the therapeutic index for drug targeting

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dc.contributor.authorRamli, Men_AU
dc.contributor.authorSmith, SVen_AU
dc.contributor.authorLindoy, LFen_AU
dc.date.accessioned2010-04-08T05:00:55Zen_AU
dc.date.accessioned2010-04-30T05:09:25Zen_AU
dc.date.available2010-04-08T05:00:55Zen_AU
dc.date.available2010-04-30T05:09:25Zen_AU
dc.date.issued2009-05en_AU
dc.date.statistics2009-05en_AU
dc.description.abstractThe 64Cu complexes of a series of mono-, bis-, and tris-tetraazamacrocycles have been prepared, and their stability in human sera has been assessed. The ligands forming the most stable Cu2+ complexes were then conjugated to the B72.3 antibody (mAb). Conditions for conjugation of the ligands to the mAb were optimized for the concentration of protein, ligand, pH, temperature, and time. The optimum moles of Cu2+ attached to the mAb were as high as 3.5 for L2 and 5.5 or 2.7 for L5, and the immunoreactivity was ≥80%. Biodistribution of the radioimmunoconjugates showed good tumor localization and target-to-background ratios that were significantly enhanced compared to those achieved with monotetraazamacrocyclic derivatives. © 2009, American Chemical Societyen_AU
dc.identifier.citationRamli, M., Smith, S. V., & Lindoy, L. F. (2009). Investigation of novel bis- and tris-tetraazamacrocycles for use in the copper-64 (Cu-64) radiolabeling of antibodies with potential to increase the therapeutic index for drug targeting. Bioconjugate Chemistry, 20(5), 868-876. doi:10.1021/bc800337den_AU
dc.identifier.govdoc1607en_AU
dc.identifier.issn1043-1802en_AU
dc.identifier.issue5en_AU
dc.identifier.journaltitleBioconjugate Chemistryen_AU
dc.identifier.pagination868-876en_AU
dc.identifier.urihttp://dx.doi.org/10.1021/bc800337den_AU
dc.identifier.urihttp://apo.ansto.gov.au/dspace/handle/10238/3112en_AU
dc.identifier.volume20en_AU
dc.language.isoenen_AU
dc.publisherAmerican Chemical Societyen_AU
dc.subjectCopper 64en_AU
dc.subjectLigandsen_AU
dc.subjectTherapyen_AU
dc.subjectAntibodiesen_AU
dc.subjectNeoplasmsen_AU
dc.subjectLabellingen_AU
dc.titleInvestigation of novel bis- and tris-tetraazamacrocycles for use in the copper-64 (Cu-64) radiolabeling of antibodies with potential to increase the therapeutic index for drug targetingen_AU
dc.typeJournal Articleen_AU
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