Radiochemistry and Preclinical PET Imaging of ⁶⁸Ga-Desferrioxamine Radiotracers Targeting Prostate-Specific Membrane Antigen.

ABSTRACT: Radiotracers incorporating the urea-based Glu-NH-C(O)-NH-Lys group have gained prominence due to their role in targeting prostate-specific membrane antigen (PSMA)-a clinical biomarker of prostate cancer. Here, the synthesis, radiolabeling, and in vitro and in vivo characterization of two ⁶⁸Ga-radiolabeled Glu-NH-C(O)-NH-Lys radiotracers conjugated to the desferrioxamine B (DFO) chelate were evaluated. Two linker groups based on amide bond and thiourea coupling chemistries were employed to develop ⁶⁸Ga-DFO-Nsucc-PSMA (⁶⁸Ga-4) and ⁶⁸Ga-DFO- pNCS-Bn-PSMA (⁶⁸Ga-7), respectively. Radiosynthesis proceeded quantitatively at room temperature with high radiochemical yields, chemical/radiochemical purities, and specific activities. Pharmacokinet

SUBMITTER: Gourni E 

PROVIDER: S-EPMC5672994 | biostudies-literature | 2017 Jan-Dec

REPOSITORIES: biostudies-literature