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

基于快速氮杂电环化反应，开发了多肽、蛋白质和抗体的高效标记方法，并将其应用于PET和无创荧光成像。建立了N-聚糖的一般固相合成，并通过他自己的“自激活”Huisgen 1，3-偶极环加成有效地制备了模拟体内“聚糖多价效应”的树枝状聚合物型簇。通过N-聚糖对蛋白质和/或活细胞表面的修饰也通过快速氮杂电环化建立。PET和非侵入性荧光成像成功地可视化了N-糖簇和N-聚糖工程化活细胞向植入活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.