Grace A. Cumbers MBMSc , Edward D. Harvey-Latham BSc(Hons) , Michael Kassiou PhD , Eryn L. Werry PhD , Jonathan J. Danon PhD
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引用次数: 0
摘要
转运蛋白(TSPO)是一种生物标记物,可通过正电子发射断层扫描(PET)对多种中枢神经系统疾病的神经炎症进行成像。临床上使用的大多数以 TSPO 为靶点的 PET 配体都存在局限性,包括亲脂性高、脱靶或与高达 30% 的人群中存在的变异 TSPO 异构体结合力差。过去十年来,研究工作的重点是开发能克服这些局限性的改良型 TSPO PET 放射性标记物。本综述对这些所谓的 "第三代 "放射性同位素在临床和临床前环境中的开发和验证进行了批判性分析。我们还对 TSPO PET 成像的未来发展方向提出了自己的观点,包括克服当前挑战和利用神经炎症性疾病分子成像新机遇的建议。
Emerging TSPO-PET Radiotracers for Imaging Neuroinflammation: A Critical Analysis
The translocator protein (TSPO) is a biomarker for imaging neuroinflammation via Positron Emission Tomography (PET) across a broad range of CNS conditions. Most clinically used PET ligands targeting TSPO have limitations, including high lipophilicity and off-target binding or poor binding to a mutated TSPO isoform present in up to 30% of the population. Research efforts over the past decade have focused on development of improved TSPO PET radiotracers that overcome these limitations. This review provides a critical analysis of the development and validation of these so-called “third-generation” radiotracers in clinical and preclinical settings. We also offer our perspective on the future directions of TSPO PET imaging, including recommendations for overcoming current challenges and capitalizing on emerging opportunities in molecular imaging for neuroinflammatory diseases.
期刊介绍:
Seminars in Nuclear Medicine is the leading review journal in nuclear medicine. Each issue brings you expert reviews and commentary on a single topic as selected by the Editors. The journal contains extensive coverage of the field of nuclear medicine, including PET, SPECT, and other molecular imaging studies, and related imaging studies. Full-color illustrations are used throughout to highlight important findings. Seminars is included in PubMed/Medline, Thomson/ISI, and other major scientific indexes.