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通过并行T₂-加权¹⁹F-MRI加速选蛋白质-连接体相互作用

Dilara Faderl¹, Ajmal Chenakkara¹, Mazin Jouda¹

¹Institute of Microstructure Technology, Karlsruhe Institute of Technology, Hermann-von-Helmholtz-Platz 1, D-76344 Eggenstein-Leopoldshafen, Germany.

Analytical chemistry

|June 3, 2024

概括

磁共振成像 (MRI) 为药物发现查提供了一种平行方法. 这项研究证明了19F-MRI用于检测蛋白质-配体结合和确定配体亲和力,提高生物化学测试的吞吐量.

科学领域:

生物物理学的生物物理.
化学生物学化学生物学
药物发现药物发现药物发现

背景情况:

配体查对于药物发现至关重要,但目前的核磁共振 (NMR) 等方法的吞吐量有限.
磁共振成像 (MRI) 提供了固有的并行性,并且可以在图像中编码参数,这表明了更高吞吐量选的潜力.

研究的目的:

探索19F-MRI的应用,以平行表征蛋白质 - 配体相互作用.
通过19F-MRI来证明对连接体结合的检测和对连接体亲和力的确定.

主要方法:

使用定制的9折样本持有器和19F-MRI线圈进行并行测量.
采用T2加权的19F-MRI检测4-三甲胺 (TFBA) 与素的结合.
通过监测TFBA位移,通过竞争测定确定非化配体的亲和力.

主要成果:

通过使用T2加权的19F-MRI成功检测到连接物结合.
通过剂量取决于TFBA的位移,证明了非化联结体亲和力的并行确定.
通过比较并行19F-T2加权的MRI图像,推导出本扎米丁 (BA) 的亲和力.

结论:

19F-MRI可实现蛋白质 - 配体相互作用的并行表征,显著增加生物化学分析的吞吐量.
这种方法对药物发现具有前景,当与超极化技术相结合时,有可能提高灵敏度.

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