Bioorthogonal chemistry for 68Ga radiolabelling of DOTA-containing compounds
Bioorthogonal chemistry for 68Ga radiolabelling of DOTA-containing compounds
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DOI：
10.1002/jlcr.3153
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发表时间：
2014-04-01
影响因子：
1.8
通讯作者：
Spivey, Alan C.
中科院分区：
文献类型：
--
作者：
Evans, Helen L.;Carroll, Laurence;Spivey, Alan C.
铜催化的点击化学是一种高度利用的技术，用于成像应用的小分子和肽的放射性标记。然而，当金属催化不是一种实际可行的途径时，这些反应的用处就不足了；例如当使用金属螯合物作为放射性配体时。在这里，我们描述了一种在DOTA螯合物存在下进行“点击式”放射化学的方法，该方法将Ga-68放射性标记技术与成熟的生物正交反应相结合，而不依赖于金属催化。
Copper-catalysed click' chemistry is a highly utilised technique for radiolabelling small molecules and peptides for imaging applications. The usefulness of these reactions falls short, however, when metal catalysis is not a practically viable route; such as when using metal chelates as radioligands. Here, we describe a method for carrying out click-type' radiochemistry in the presence of DOTA chelates, by combining Ga-68 radiolabelling techniques with well-established bioorthogonal reactions, which do not rely upon metal catalysis.