生物正交化学
点击化学
化学
叠氮化物
聚糖
生物化学
离体
体内
共轭体系
组织蛋白酶B
组合化学
生物
体外
酶
生物技术
有机化学
糖蛋白
聚合物
作者
Man Kyu Shim,Hong Yeol Yoon,Ju Hee Ryu,Heebeom Koo,Sang‐Min Lee,Jae Hyung Park,Jong‐Ho Kim,Seulki Lee,Martin G. Pomper,Ick Chan Kwon,Kwangmeyung Kim
标识
DOI:10.1002/anie.201608504
摘要
Abstract Recently, metabolic glycoengineering with bioorthogonal click reactions has focused on improving the tumor targeting efficiency of nanoparticles as delivery vehicles for anticancer drugs or imaging agents. It is the key technique for developing tumor‐specific metabolic precursors that can generate unnatural glycans on the tumor‐cell surface. A cathepsin B‐specific cleavable substrate (KGRR) conjugated with triacetylated N ‐azidoacetyl‐ d ‐mannosamine (RR‐S‐Ac 3 ManNAz) was developed to enable tumor cells to generate unnatural glycans that contain azide groups. The generation of azide groups on the tumor cell surface was exogenously and specifically controlled by the amount of RR‐S‐Ac 3 ManNAz that was fed to target tumor cells. Moreover, unnatural glycans on the tumor cell surface were conjugated with near infrared fluorescence (NIRF) dye‐labeled molecules by a bioorthogonal click reaction in cell cultures and in tumor‐bearing mice. Therefore, our RR‐S‐Ac 3 ManNAz is promising for research in tumor‐specific imaging or drug delivery.
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