In order to demonstrate utility of the CuAAC/demetallation tandem reaction for assembly of large multimeric bioconjugates and application in the design of therapeutic radiopharmaceuticals, the 4-fold azide-decorated building block DOTPI(azide)4 (Wurzer et al., 2018) was reacted with alkyne-functionalized KuE (lysine-urea-glutamic acid, an inhibitor motif for prostate-specific membrane antigen, PSMA, EC 3.4.17.21; synonyms: glutamate carboxypeptidase II, NAALADase (Mesters et al., 2006); a membrane-bound zinc hydrolase which is overexpressed by malignant human prostate cancers). This evidence concerns the gene FOLH1 and prostate carcinoma.