Immunomedics, Inc., Morris Plains, New Jersey 07950, USA.
Bioconjug Chem. 2010 Jul 21;21(7):1331-40. doi: 10.1021/bc100137x.
We reported previously the feasibility to radiolabel peptides with fluorine-18 ((18)F) using a rapid one-pot method that first mixes (18)F(-) with Al(3+) and then binds the (Al(18)F)(2+) complex to a NOTA ligand on the peptide. In this report, we examined several new NOTA ligands and determined how temperature, reaction time, and reagent concentration affected the radiolabeling yield. Four structural variations of the NOTA ligand had isolated radiolabeling yields ranging from 5.8% to 87% under similar reaction conditions. All of the Al(18)F NOTA complexes were stable in vitro in human serum, and those that were tested in vivo also were stable. The radiolabeling reactions were performed at 100 degrees C, and the peptides could be labeled in as little as 5 min. The IMP467 peptide could be labeled up to 115 GBq/micromol (3100 Ci/mmol), with a total reaction and purification time of 30 min without chromatographic purification.
我们曾报道过使用氟-18（18F）对肽进行放射性标记的可行性，采用一种快速的一锅法，首先将 18F-与 Al3+混合，然后将（Al18F）2+配合物结合到肽上的 NOTA 配体上。在本报告中，我们研究了几种新的 NOTA 配体，并确定了温度、反应时间和试剂浓度如何影响放射性标记产率。在相似的反应条件下，NOTA 配体的四个结构变体的分离放射性标记产率范围为 5.8%至 87%。所有的 Al18F NOTA 配合物在人血清中体外稳定，在体内测试的那些也稳定。放射性标记反应在 100°C 下进行，肽的标记时间可以短至 5 分钟。IMP467 肽的放射性标记最高可达 115GBq/µmol（3100Ci/mmol），总反应和纯化时间为 30 分钟，无需色谱纯化。
