In vitro binding analysis of THK523 to Aβ and tau protein fibrils
Tuesday, Nov 15, 2011, 11:00 AM -12:00 PM
, N. OKAMURA
, S. FURUMOTO
, T. YOSHIKAWA
, H. ARAI
, Y. KUDO
, *K. YANAI
Dept Geriatrics and Gerontology, Tohoku Univ. Sch. Med., Sendai, Japan;
Innovation of New Biomed. Engin. Ctr., Tohoku Univ., Sendai, Japan
The deposition of senile plaques (SPs) and neurofibrillary tangles (NFTs) represents a pathological hallmark of Alzheimer’s disease (AD). Recent advances in the development of PET imaging radiotracers such as [
C]Pittsburgh Compound-B (PiB), and [
C]BF-227, resulted in successful detection of amyloid deposition in the living human brains. Recently we developed a novel ligand, [
F]THK-523, for in vivo imaging of tau proteins. In this study, we compared the binding properties of THK-523 to synthetic protein fibrils and human brain tissue with amyloid imaging probes such as BF-227 and FDDNP.
In vitro radioligand binding assays were conducted using synthetic Aβ
and K18ΔK280 tau fibrils. Non-specific binding was determined by the mixture of 2 μM unlabeled compounds. In vitro autoradiography was conducted using AD hippocampal brain sections to examine the radioligand binding to neuropathological lesions.
In vitro binding assay indicated that [
F]THK-523 bound to tau fibrils with higher affinity than Aβ
fibrils, while [
F]BF-227 bound to Aβ
fibrils with higher affinity than that to tau
fibrils. Autoradiographic analysis indicated that [
F]THK-523 accumulated in CA1 region of AD hippocampus, which contains high density of tau deposits. On the other hand, [
F]BF-227 accumulated in the region which contains high density amyloid burden. [
F]FDDNP showed low binding affinity to both Aβ
and tau fibrils and did not show any significant accumulation in AD hippocampus.
This study demonstrated the unique binding property of [
F]THK-523, suggesting the usefulness of this probe for selective identification of tau pathology in AD brain.
Positron Emission Tomography
[Authors]. [Abstract Title]. Program No. XXX.XX. 2011 Neuroscience Meeting Planner. Washington, DC: Society for Neuroscience, 2011. Online.
2011 Copyright by the Society for Neuroscience all rights reserved. Permission to republish any abstract or part of any abstract in any form must be obtained in writing by SfN office prior to publication.
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