Simple and convenient radiolabeling of proteins using a prelabeling-approach with thiol-DOTA |
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Authors: | Carmen Wängler Ralf Schirrmacher Peter Bartenstein Björn Wängler |
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Institution: | 1. McConnell Brain Imaging Center, Montreal Neurological Institute, McGill University, University Street 3800, Montreal H3A 2B4, Quebec, Canada;2. University Hospital Munich, Department of Nuclear Medicine, Ludwig-Maximilians-University, Marchioninistraße 15, Munich, Germany |
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Abstract: | Commonly applied methods for radiometal-labeling of proteins require complex and protracted derivatization reactions of the protein and the subsequent radiolabeling is time-consuming due to the low reaction temperatures applicable. Therefore, a convenient and efficient prelabeling technique for proteins using the DOTA derivative 2,2′,2′′-(10-(2-(2-mercaptoethylamino)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetic acid (thiol-DOTA) containing a thiol moiety for rapid and selective introduction into maleimide-derivatized proteins was developed. Thiol-DOTA was labeled with 68Ga, 90Y and 177Lu and subsequently introduced into bovine serum albumin and a human IgG with maximum radiochemical yields of 66%. The entire radiolabeling procedure was completed after only 30 min making this a favorable new labeling technique for proteins. |
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