Development of PET Imaging through Rapid Azaelectrocyclization and Oligosaccharide-Engineered Functional Macromolecules

基于快速氮杂电环反应，发展了多肽、蛋白质和抗体的高效标记，并将该方法应用于PET和非侵入性荧光成像。建立了N-葡聚糖的通用固载合成方法，并通过自激活的惠斯根1，3-偶极环加成反应有效地制备了模拟体内“多价糖效应”的树状大分子簇合物。蛋白质和/或活细胞表面的N-葡聚糖修饰也是通过快速氮杂电环反应建立的。PET和非侵入性荧光成像成功地显示了N-糖簇和N-糖工程活细胞向植入活体动物体内的特定器官和/或肿瘤的运输。

Efficient labeling of peptides, proteins, and antibodies were developed based on the rapid azaelectrocyclization, and the method was applied to the PET and the noninvasive fluorescence imaging. General solid-supported synthesis of N-glycans was established and their dendrimer-type clusters, mimicking the "glycan multivalency effects" in vivo, were efficiently prepared by his own "self-activating" Huisgen 1,3-dipolar cycloaddition. Modification of the proteins and/or the living cell surfaces by N-glycans were also established by rapid azaelectrocyclization. PET and noninvasive fluorescence imaging successfully visualized the trafficking of N-glycoclusters and N-glycan-engineered living cells to the specific organs and/or tumors implanted in living animals.