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tau正电子发射断层扫描(PET)成像:过去、现在与未来

Tau Positron Emission Tomography (PET) Imaging: Past, Present, and Future.

作者信息

Ariza Manuela, Kolb Hartmuth C, Moechars Dieder, Rombouts Frederik, Andrés José Ignacio

机构信息

†Neuroscience Medicinal Chemistry, Janssen Research and Development, a Division of Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium.

‡Neuroscience Biomarkers, Janssen Research and Development, 3210 Merryfield Row, San Diego, California 92121, United States.

出版信息

J Med Chem. 2015 Jun 11;58(11):4365-82. doi: 10.1021/jm5017544. Epub 2015 Feb 25.

Abstract

Alzheimer's disease (AD) is a chronic neurodegenerative disorder and the most common cause of dementia among the elderly population. The good correlation of the density and neocortical spread of neurofibrillary tangles (NFTs) with clinical AD disease progression offers an opportunity for the early diagnosis and staging using a noninvasive imaging technique such as positron emission tomography (PET). Thus, PET imaging of NFTs not only holds promise as a diagnostic tool but also may enable the development of disease modifying therapeutics for AD. In this review, we focus on the structural diversity of tau PET tracers, the challenges related to the identification of high affinity and highly selective NFT ligands, and recent progress in the clinical development of tau PET radioligands.

摘要

阿尔茨海默病(AD)是一种慢性神经退行性疾病,也是老年人群中痴呆最常见的病因。神经原纤维缠结(NFTs)的密度和新皮质扩散与临床AD疾病进展具有良好的相关性,这为使用正电子发射断层扫描(PET)等非侵入性成像技术进行早期诊断和分期提供了机会。因此,NFTs的PET成像不仅有望成为一种诊断工具,还可能推动AD疾病修饰疗法的发展。在本综述中,我们重点关注tau PET示踪剂的结构多样性、与高亲和力和高选择性NFT配体鉴定相关的挑战,以及tau PET放射性配体临床开发的最新进展。

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