Department of Radiology, University of Michigan, Ann Arbor, Michigan 48109, United States.
ACS Chem Neurosci. 2022 Oct 5;13(19):2778-2783. doi: 10.1021/acschemneuro.2c00519. Epub 2022 Sep 16.
Imaging of misfolded proteins implicated in neurodegenerative disorders using positron emission tomography (PET) imaging has revolutionized dementia research. In this viewpoint, the development of radiotracers for tau PET is highlighted. We draw attention to key innovations that were essential to development of radiotracers for imaging tau, from early imaging agents, through the structure-activity relationship (SAR) studies required to minimize off-target binding of the newer probes in use today. We also highlight development of Tauvid, the first tau PET radiotracer approved by the US FDA for tau imaging in adult patients with cognitive impairment who are being evaluated for Alzheimer's disease.
正电子发射断层扫描(PET)成像技术对错误折叠的蛋白质进行成像,用于神经退行性疾病的研究,从而引发了一场革命。在本观点中,我们强调了用于 tau PET 的放射性示踪剂的发展。我们提请注意对 tau 成像的放射性示踪剂的发展至关重要的关键创新,从早期的成像剂,到今天使用的新型探针的最小化非靶标结合的结构活性关系(SAR)研究。我们还强调了 Tauvid 的开发,这是第一个由美国 FDA 批准的用于 tau 成像的放射性示踪剂,用于评估认知障碍的成年患者的阿尔茨海默病。