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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Tetrazine-trans-cyclooctene ligation for the rapid construction of integrin alphavbeta targeted PET tracer based on a cyclic RGD peptide.
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Tetrazine-trans-cyclooctene ligation for the rapid construction of integrin alphavbeta targeted PET tracer based on a cyclic RGD peptide.

机译：Tetrazine-反式-环辛烯连接用于基于环状RGD肽的整合素αvbeta靶向PET示踪剂的快速构建。

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摘要

Labeling biomolecules with (18)F is usually done through coupling with prosthetic groups, which generally requires several time-consuming radiosynthetic steps resulting in low labeling yield. Recently, the tetrazine-trans-cyclooctene ligation has been introduced as a method of bioconjugation that proceeds with fast reaction rates without need for catalysis. Herein, we report the development of an extremely fast and efficient method for generating (18)F labeled probes based on the tetrazine-trans-cyclooctene ligation. Starting with only 30 mug (78 muM) of a tetrazine-RGD conjugate and 2 mCi (5 muM) of (18)F-trans-cyclooctene, the (18)F labeled RGD peptide could be obtained in more than 90% yield within five minutes. The (18)F labeled RGD peptide demonstrated prominent tumor uptake in vivo. The receptor specificity was confirmed by blocking experiments. These results successfully demonstrate that the tetrazine-trans-cyclooctene ligation serves as an efficient labeling method for PET probe construction.
机译：用（18）F标记生物分子通常是通过与修复基团偶联来完成的，这通常需要几个耗时的放射合成步骤，导致标记产率低。近来，已经引入四嗪-反式-环辛烯连接作为生物缀合的方法，其以快速的反应速率进行而无需催化。在本文中，我们报告了基于四嗪-反式-环辛烯连接的一种非常快速有效的方法，用于生成（18）F标记的探针。仅从30杯（78μM）四嗪-RGD共轭物和2 mCi（5μM）（18）F-反式-环辛烯开始，可以在90％的产率下获得（18）F标记的RGD肽5分钟。 （18）F标记的RGD肽在体内表现出显着的肿瘤吸收。通过阻断实验证实了受体特异性。这些结果成功地证明了四嗪-反式-环辛烯的连接可作为PET探针构建的有效标记方法。

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