铜（I）辅助的点击化学策略用于将未保护的交联大环螯合剂与肿瘤靶向肽偶联。
Cu(I)-assisted click chemistry strategy for conjugation of non-protected cross-bridged macrocyclic chelators to tumour-targeting peptides.
作者信息
Cai Zhengxin, Li Barbara T Y, Wong Edward H, Weisman Gary R, Anderson Carolyn J
机构信息
Department of Radiology, University of Pittsburgh, Pittsburgh, PA, USA.
出版信息
Dalton Trans. 2015 Mar 7;44(9):3945-8. doi: 10.1039/c4dt03897e.
Abstract
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.
摘要
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。
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