Department of Radiology, Carver College of Medicine, The University of Iowa, 500 Newton Road, ML B180, Iowa City, IA 52242, USA.
Bioorg Med Chem Lett. 2011 Oct 1;21(19):5757-61. doi: 10.1016/j.bmcl.2011.08.017. Epub 2011 Aug 8.
Radionuclide chelators (DOTA, NOTA) functionalized with a monofluorocyclooctyne group were prepared. These materials reacted rapidly and in high yield with a fully deprotected azide-modified peptide via Cu-free click chemistry under mild reaction conditions (aqueous solution, room temperature). The resulting bioconjugates bind with high affinity and specificity to their cell-surface receptor targets in vitro and appear stable to degradation in mouse serum over 3h of incubation at 37°C.
放射性核素螯合剂（DOTA、NOTA）被官能化带有单氟环辛炔基团。这些材料在温和的反应条件下（水溶液，室温），通过无铜点击化学反应，快速且高产地与完全去保护的叠氮化物修饰肽反应。所得的生物缀合物在体外与细胞表面受体靶标具有高亲和力和特异性结合，并且在 37°C 孵育 3 小时的情况下，在小鼠血清中似乎稳定，不易降解。
