Radiosynthesis and evaluation of a novel ¹⁸F-labeled tracer for PET imaging of glycogen synthase kinase 3.

IF 2 Q3 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING

American journal of nuclear medicine and molecular imaging Pub Date : 2024-10-15 eCollection Date: 2024-01-01 DOI:10.62347/OBZS8887

Zhiwei Xiao, Yinlong Li, Ahmed Haider, Stefanie K Pfister, Jian Rong, Jiahui Chen, Chunyu Zhao, Xin Zhou, Zhendong Song, Yabiao Gao, Jimmy S Patel, Thomas L Collier, Chongzhao Ran, Chuangyan Zhai, Hongjie Yuan, Steven H Liang

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引用次数: 0

Abstract

Glycogen synthase kinase 3 (GSK3) is a multifunctional serine/threonine kinase family that regulates diverse biological processes including glucose metabolism, insulin activity and energy homeostasis. Dysregulation of GSK3 is implicated in the development of several diseases such as type 2 diabetes mellitus, Alzheimer's disease (AD), and various cancer types. In this study, we report the synthesis and evaluation of a novel positron emission tomography (PET) ligand compound 28 (codenamed [¹⁸F]GSK3-2209). The PET ligand [¹⁸F]28 was obtained via copper-mediated radiofluorination in more than 32% radiochemical yields, with high radiochemical purity and high molar activity. In vitro autoradiography studies in rodents demonstrated that this tracer exhibited a high specific binding to GSK3. Furthermore, PET imaging studies of [¹⁸F]28 revealed its ability to penetrate the blood-brain barrier (BBB).

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用于糖原合酶激酶 3 PET 成像的新型 18F 标记示踪剂的放射合成与评估。

糖原合酶激酶 3（GSK3）是一个多功能丝氨酸/苏氨酸激酶家族，它调控多种生物过程，包括葡萄糖代谢、胰岛素活性和能量平衡。GSK3 的失调与多种疾病的发生有关，如 2 型糖尿病、阿尔茨海默病（AD）和各种癌症。在这项研究中，我们报告了新型正电子发射断层扫描（PET）配体化合物 28（代号为 [18F]GSK3-2209）的合成和评估。PET 配体[18F]28 是通过铜介导的放射氟化反应获得的，放射化学收率超过 32%，具有高放射化学纯度和高摩尔活性。啮齿动物体外自显影研究表明，这种示踪剂与 GSK3 具有高度特异性结合。此外，[18F]28 的 PET 成像研究表明，它能够穿透血脑屏障（BBB）。

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来源期刊

American journal of nuclear medicine and molecular imaging RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING-

自引率

4.00%

发文量

期刊介绍： The scope of AJNMMI encompasses all areas of molecular imaging, including but not limited to: positron emission tomography (PET), single-photon emission computed tomography (SPECT), molecular magnetic resonance imaging, magnetic resonance spectroscopy, optical bioluminescence, optical fluorescence, targeted ultrasound, photoacoustic imaging, etc. AJNMMI welcomes original and review articles on both clinical investigation and preclinical research. Occasionally, special topic issues, short communications, editorials, and invited perspectives will also be published. Manuscripts, including figures and tables, must be original and not under consideration by another journal.