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Tetrazine-Derived Near-Infrared Dye as a Facile Reagent for Developing Targeted Photoacoustic Imaging Agents.
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2020-07-22 , DOI: 10.1021/acs.molpharmaceut.0c00441 Samantha Slikboer 1 , Zoya Naperstkow 1 , Nancy Janzen 1 , Amber Faraday 1 , Yohannes Soenjaya 2 , Johann Le Floc'h 2 , Salma Al-Karmi 1 , Rowan Swann 1 , Kevin Wyszatko 1 , Christine E M Demore 2 , Stuart Foster 2 , John F Valliant 1
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2020-07-22 , DOI: 10.1021/acs.molpharmaceut.0c00441 Samantha Slikboer 1 , Zoya Naperstkow 1 , Nancy Janzen 1 , Amber Faraday 1 , Yohannes Soenjaya 2 , Johann Le Floc'h 2 , Salma Al-Karmi 1 , Rowan Swann 1 , Kevin Wyszatko 1 , Christine E M Demore 2 , Stuart Foster 2 , John F Valliant 1
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A new photoacoustic (PA) dye was developed as a simple-to-use reagent for creating targeted PA imaging agents. The lead molecule was prepared via an efficient two-step synthesis from an inexpensive commercially available starting material. With the dye’s innate albumin-binding properties, the resulting tetrazine-derived dye is capable of localizing to tumor and exhibits a biological half-life of a few hours, allowing for an optimized distribution profile. The presence of tetrazine in turn makes it possible to link the albumin-binding optoacoustic signaling agent to a wide range of targeting molecules. To demonstrate the utility and ease of use of the platform, a novel PA probe for imaging calcium accretion was generated using a single-step bioorthogonal coupling reaction where high-resolution PA images of the knee joint in mice were obtained as early as 1 h post injection. Whole-body distribution was subsequently determined by labeling the probe with 99mTc and performing tissue counting following necropsy. These studies, along with tumor imaging and in vitro albumin binding studies, revealed that the core PA contrast agent can be imaged in vivo and can be easily linked to targeting molecules for organ-specific uptake.
中文翻译：
特特拉津衍生的近红外染料作为用于开发目标光声成像剂的简便试剂。
一种新的光声（PA）染料被开发为一种易于使用的试剂，可用于生成目标PA成像剂。铅分子是通过一种有效的两步合成法，由一种廉价的可商购原料制备的。具有染料固有的白蛋白结合特性，所得的四嗪衍生染料能够定位于肿瘤，并具有数小时的生物学半衰期，从而实现了最佳的分布特性。反之，四嗪的存在使得将结合白蛋白的光声信号传导剂与多种靶向分子连接成为可能。为了演示该平台的实用性和易用性，使用单步生物正交偶联反应生成了一种新型的用于钙累积成像的PA探针，其中在注射后1 h即可获得小鼠膝关节的高分辨率PA图像。随后通过将探针标记为来确定全身分布99m Tc，尸检后进行组织计数。这些研究以及肿瘤成像和体外白蛋白结合研究表明，核心PA造影剂可以在体内成像，并且可以轻松地与靶向分子结合以进行器官特异性摄取。
更新日期：2020-09-09
中文翻译：
特特拉津衍生的近红外染料作为用于开发目标光声成像剂的简便试剂。
一种新的光声（PA）染料被开发为一种易于使用的试剂，可用于生成目标PA成像剂。铅分子是通过一种有效的两步合成法，由一种廉价的可商购原料制备的。具有染料固有的白蛋白结合特性，所得的四嗪衍生染料能够定位于肿瘤，并具有数小时的生物学半衰期，从而实现了最佳的分布特性。反之，四嗪的存在使得将结合白蛋白的光声信号传导剂与多种靶向分子连接成为可能。为了演示该平台的实用性和易用性，使用单步生物正交偶联反应生成了一种新型的用于钙累积成像的PA探针，其中在注射后1 h即可获得小鼠膝关节的高分辨率PA图像。随后通过将探针标记为来确定全身分布99m Tc，尸检后进行组织计数。这些研究以及肿瘤成像和体外白蛋白结合研究表明，核心PA造影剂可以在体内成像，并且可以轻松地与靶向分子结合以进行器官特异性摄取。
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