Tetrazine—trans-Cyclooctene Chemistry Applied to Fabricate Self-Assembled Fluorescent and Radioactive Nanoparticles for in Vivo Dual Mode Imaging,Bioconjugate Chemistry

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Tetrazine—trans-Cyclooctene Chemistry Applied to Fabricate Self-Assembled Fluorescent and Radioactive Nanoparticles for in Vivo Dual Mode Imaging
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2019-02-07 00:00:00 , DOI: 10.1021/acs.bioconjchem.9b00038
Arthur H A M van Onzen ₁ , Raffaella Rossin ₂ , Albertus P H J Schenning ₃ , Klaas Nicolay ₄ , Lech-Gustav Milroy ₁ , Marc S Robillard ₂ , Luc Brunsveld ₁

Affiliation

Multimodal imaging agents combine two or more imaging modalities into one probe. Self-assembling fluorescent nanoparticles are a promising class of modular multimodal imaging probes as they can allow easy blending of imaging and targeting modalities. Our group recently developed a class of self-assembling and intrinsically fluorescent small molecule-based nanoparticles (SMNPs) with excellent optical properties. In this article, we describe the efficient radiolabeling of these SMNPs via a two-step bioconjugation strategy involving the inverse-electron-demand Diels–Alder ligation between a tetrazine (Tz)-tagged radiolabel and a trans-cyclooctene (TCO)-tagged fluorescent small molecule building block of the SMNPs. Studies in mice revealed that the SMNPs are well tolerated and could be monitored by both radioactivity and fluorescence, thereby demonstrating the potential of SMNPs in optical and dual-mode imaging in vivo. The work also testifies to the utility of the Tz–TCO conjugation chemistry for the labeling of self-assembled nanoparticles.

中文翻译：

四嗪—反式环辛烯化学用于制造用于体内双模式成像的自组装荧光和放射性纳米颗粒

多模态成像剂将两种或多种成像方式组合到一个探针中。自组装荧光纳米粒子是一类有前途的模块化多模态成像探针，因为它们可以轻松混合成像和靶向模式。我们的团队最近开发了一类具有优异光学特性的自组装和本质荧光小分子纳米颗粒（SMNP）。在本文中，我们描述了通过两步生物共轭策略对这些 SMNP 进行有效的放射性标记，该策略涉及四嗪 (Tz) 标记的放射性标记和反式环辛烯 (TCO) 标记的荧光标记之间的反电子需求 Diels-Alder连接。 SMNP 的小分子构建块。对小鼠的研究表明，SMNP 具有良好的耐受性，并且可以通过放射性和荧光进行监测，从而证明了 SMNP 在体内光学和双模式成像中的潜力。这项工作还证明了 Tz-TCO 共轭化学在标记自组装纳米粒子方面的实用性。

更新日期：2019-02-07

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