Radiolabelling of isopeptide Nε-(γ-glutamyl)-L-lysine by conjugation with N-succinimidyl-4-[18F]fluorobenzoate
Radiolabelling of isopeptide Nε-(γ-glutamyl)-L-lysine by conjugation with N-succinimidyl-4-[18F]fluorobenzoate
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DOI：
10.1016/s0969-8043(03)00161-1
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发表时间：
2003-07-01
影响因子：
1.6
通讯作者：
Henle, T
中科院分区：
文献类型：
--
作者：
Wüst, F;Hultsch, C;Henle, T
异肽n- ε -（γ -谷氨酰基）- l-赖氨酸4通过n-琥珀酰酰-4-[F-18]氟苯甲酸酯（[F-18]SFB）用F-18标记。采用一种改进的方法方便地合成[F-18]SFB，在EOB后40 min内，[F-18]SFB的衰变校正放射化学产率为44-53% (n=20)，放射化学纯度为>95%。用[F-18]SFB标记n- ε -（γ -谷氨酰）- l -赖氨酸，研究了异肽浓度、温度和pH的影响，确定了最佳反应条件。偶联反应不受温度和pH的影响，但受异肽浓度的影响较大。在优化的标记条件下，在典型实验中，1.3 GBq [F-18]SFB可在45 min内转化为447MBq（46%，衰减校正）的[F-18]氟苯甲酰化异肽，包括HPLC纯化。(C) 2003 Elsevier Ltd.版权所有。
The isopeptide N-epsilon-(gamma-glutamyl)-L-lysine 4 was labelled with F-18 via N-succinimidyl-4-[F-18]fluorobenzoate ([F-18]SFB). A modified approach for the convenient synthesis of [F-18]SFB was used, and [F-18]SFB could be obtained in decay-corrected radiochemical yields of 44-53% (n=20) and radiochemical purity >95% within 40 min after EOB. For labelling N-epsilon-(gamma-glutamyl)-L-lysine with [F-18]SFB the effects of isopeptide concentration, temperature, and pH were studied to determine the optimum reaction conditions. The coupling reaction was shown to be temperature and pH independent while being strongly affected by the isopeptide concentration. Using the optimized labelling conditions, in a typical experiment 1.3 GBq of [F-18]SFB could be converted into 447MBq (46%, decay-corrected) of [F-18]fluorobenzoylated isopeptide within 45 min, including HPLC purification. (C) 2003 Elsevier Ltd. All rights reserved.