Cai Zhengxin, Li Barbara T Y, Wong Edward H, Weisman Gary R, Anderson Carolyn J
Department of Radiology, University of Pittsburgh, Pittsburgh, PA, USA.
Dalton Trans. 2015 Mar 7;44(9):3945-8. doi: 10.1039/c4dt03897e.
Copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) click chemistry has inherent challenges for copper-labeled radiopharmaceuticals. An azide-modified phosphonate-based cross-bridged macrocyclic chelator was synthesized for click chemistry conjugation with azide-modified Y3-TATE (a somatostatin analogue) on resin, without the need for protecting the chelator. The (64)Cu-labeled bioconjugate shows favourable in vitro and in vivo behaviour.
铜（I）催化的叠氮化物-炔烃环加成（CuAAC）点击化学对于铜标记的放射性药物存在内在挑战。合成了一种叠氮化物修饰的基于膦酸酯的交联大环螯合剂，用于在树脂上与叠氮化物修饰的Y3-TATE（一种生长抑素类似物）进行点击化学偶联，无需保护螯合剂。（64）Cu标记的生物共轭物表现出良好的体外和体内行为。
