Fast Fluorine-18 labeling and preclinical evaluation of novel Mucin1 and its Folate hybrid peptide conjugate for targeting breast carcinoma

Abstract Background There is a need to develop new and more potent radiofluorinated peptide their hybrid conjugates for multiple-receptors targeting properties that overexpress on many cancers. Methods We have synthesized MUC1-[ 18 F] SFB MUC1-FA-[ using convenient one-step nucleophilic displacement reaction. In vitro cell binding in vivo evaluation animals were performed determine the potential of these radiolabeled compounds. Results Radiochemical yields greater than 70% less 30 min synthesis time. purities 97% without HPLC purification, which makes approaches amenable automation. studies MCF7 breast cancer cells showed significant amounts associated with fractions held good affinity specificity cells. characterization Balb/c mice revealed rapid blood clearance excretion predominantly by urinary as well hepatobiliary systems MUC1-[18F] MUC1-FA-[18F] SFB, respectively. Biodistribution SCID bearing xenografts, demonstrated excellent tumor uptake (12% ID/g) favorable kinetics over F]SFB. The was blocked excess co-injection cold peptides suggesting receptor-mediated process. Conclusion Initial PET/CT imaging confirmed observations. These results demonstrate may be useful PET probe detection monitoring response treatment.