18F-Labeled 2-Arylquinoline Derivatives for Tau Imaging: Chemical, Radiochemical, Biological and Clinical Features

Author(s): Shozo Furumoto, Tetsuro Tago, Ryuichi Harada, Yukitsuka Kudo, Nobuyuki Okamura.

Journal Name: Current Alzheimer Research

Volume 14 , Issue 2 , 2017

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Alzheimer’s disease is the most common form of dementia among older people. Misfolding and aggregation of proteins (amyloid-β and tau) in the brain is the primary cause of neurodegeneration in the disease. Non-invasive detection of amyloid-β deposition can be realized using positron emission tomography probes, but a proportion of Aβ-positive subjects do not present with cognitive dysfunction, suggesting limitations in assessment using this method. Non-invasive detection of tau deposits in the brain can be used to diagnose, monitor, and predict Alzheimer’s disease progression. Tau positron emission tomography radiolabelled probes such as T807, THK-5117, and PBB3 can image the pathology of the disease in vivo. The 18F-labeled tau imaging agents 18F-THK-5351, 18F-T807 (18F-AV-1451), and 18F-RO6958948 are presently under evaluation in clinical studies and clinical trials worldwide. This imaging methodology could be applied to enable preclinical diagnoses and disease-modifying drugs for Alzheimer’s disease. In this review, we provide an overview of the pathology and potential imaging of tau in Alzheimer’s disease, development of a THK series among tau tracers, and the chemical, radiochemical, biological, and clinical features of tau probes.

Keywords: Alzheimer’s disease, aggregation, brain, amyloid-β, tau, positron emission tomography, THK series, protein.

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Year: 2017
Page: [178 - 185]
Pages: 8
DOI: 10.2174/1567205013666160620121811
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