Syk inhibitors reduce tau protein phosphorylation and oligomerization

Spleen tyrosine kinase (Syk), a non-receptor-type tyrosine kinase, has a wide range of physiological functions. A possible role of Syk in Alzheimer's disease (AD) has been proposed. We evaluated the localization of Syk in the brains of patients with AD and control participants. Human neuroblast...

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Main Authors: Tomohisa Yamaguchi, Tadanori Hamano, Kiyonao Sada, Rei Asano, Nicholas M. Kanaan, Hirohito Sasaki, Shu-Hui Yen, Yuki Kitazaki, Yoshinori Endo, Soichi Enomoto, Norimichi Shirafuji, Masamichi Ikawa, Osamu Yamamura, Youshi Fujita, Koji Aoki, Hironobu Naiki, Maho Morishima, Yuko Saito, Shigeo Murayama, Yasunari Nakamoto
Format: Article
Language:English
Published: Elsevier 2024-10-01
Series:Neurobiology of Disease
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Online Access:http://www.sciencedirect.com/science/article/pii/S0969996124002560
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author Tomohisa Yamaguchi
Tadanori Hamano
Kiyonao Sada
Rei Asano
Nicholas M. Kanaan
Hirohito Sasaki
Shu-Hui Yen
Yuki Kitazaki
Yoshinori Endo
Soichi Enomoto
Norimichi Shirafuji
Masamichi Ikawa
Osamu Yamamura
Youshi Fujita
Koji Aoki
Hironobu Naiki
Maho Morishima
Yuko Saito
Shigeo Murayama
Yasunari Nakamoto
author_facet Tomohisa Yamaguchi
Tadanori Hamano
Kiyonao Sada
Rei Asano
Nicholas M. Kanaan
Hirohito Sasaki
Shu-Hui Yen
Yuki Kitazaki
Yoshinori Endo
Soichi Enomoto
Norimichi Shirafuji
Masamichi Ikawa
Osamu Yamamura
Youshi Fujita
Koji Aoki
Hironobu Naiki
Maho Morishima
Yuko Saito
Shigeo Murayama
Yasunari Nakamoto
author_sort Tomohisa Yamaguchi
collection DOAJ
description Spleen tyrosine kinase (Syk), a non-receptor-type tyrosine kinase, has a wide range of physiological functions. A possible role of Syk in Alzheimer's disease (AD) has been proposed. We evaluated the localization of Syk in the brains of patients with AD and control participants. Human neuroblastoma M1C cells harboring wild-type tau (4R0N) were used with the tetracycline off (TetOff) induction system. In this model of neuronal tauopathy, the effects of the Syk inhibitors—BAY 61–3606 and R406—on tau phosphorylation and oligomerization were explored using several phosphorylated tau-specific antibodies and an oligomeric tau antibody, and the effects of these Syk inhibitors on autophagy were examined using western blot analyses. Moreover, the effects of the Syk inhibitor R406 were evaluated in vivo using wild-type mice. In AD brains, Syk and phosphorylated tau colocalized in the cytosol. In M1C cells, Syk protein (72 kDa) was detected using western blot analysis. Syk inhibitors decreased the expression levels of several tau phosphoepitopes including PHF-1, CP13, AT180, and AT270. Syk inhibitors also decreased the levels of caspase-cleaved tau (TauC3), a pathological tau form. Syk inhibitors increased inactivated glycogen synthase kinase 3β expression and decreased active p38 mitogen-activated protein kinase expression and demethylated protein phosphatase 2 A levels, indicating that Syk inhibitors inactivate tau kinases and activate tau phosphatases. Syk inhibitors also activated autophagy, as indicated by increased LC3II and decreased p62 levels. In vivo, the Syk inhibitor R406 decreased phosphorylated tau levels in wild-type mice. These findings suggest that Syk inhibitors offer novel therapeutic strategies for tauopathies, including AD.
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spelling doaj-art-239a93f919264675ad69ceb404dfc1d22025-08-20T01:48:03ZengElsevierNeurobiology of Disease1095-953X2024-10-0120110665610.1016/j.nbd.2024.106656Syk inhibitors reduce tau protein phosphorylation and oligomerizationTomohisa Yamaguchi0Tadanori Hamano1Kiyonao Sada2Rei Asano3Nicholas M. Kanaan4Hirohito Sasaki5Shu-Hui Yen6Yuki Kitazaki7Yoshinori Endo8Soichi Enomoto9Norimichi Shirafuji10Masamichi Ikawa11Osamu Yamamura12Youshi Fujita13Koji Aoki14Hironobu Naiki15Maho Morishima16Yuko Saito17Shigeo Murayama18Yasunari Nakamoto19Second Department of Internal Medicine, Faculty of Medical Sciences, University of Fukui, Fukui, JapanSecond Department of Internal Medicine, Faculty of Medical Sciences, University of Fukui, Fukui, Japan; Department of Aging and Dementia (DAD), Faculty of Medical Sciences, University of Fukui, Fukui, Japan; Life Science Innovation Center, University of Fukui, Fukui, Japan; Corresponding author at: Second Department of Internal Medicine, University of Fukui, 23-3 Matsuokashimoaizuki, Eiheiji, Fukui 910-1193, Japan.Department of Genome Science and Microbiology, Faculty of Medical Sciences, University of Fukui, Fukui, JapanSecond Department of Internal Medicine, Faculty of Medical Sciences, University of Fukui, Fukui, JapanDepartment of Translational Neuroscience, College of Human Medicine, Michigan State University, MI, USASecond Department of Internal Medicine, Faculty of Medical Sciences, University of Fukui, Fukui, JapanDepartment of Neuroscience, Mayo Clinic Jacksonville, FL, USASecond Department of Internal Medicine, Faculty of Medical Sciences, University of Fukui, Fukui, JapanSecond Department of Internal Medicine, Faculty of Medical Sciences, University of Fukui, Fukui, JapanSecond Department of Internal Medicine, Faculty of Medical Sciences, University of Fukui, Fukui, JapanSecond Department of Internal Medicine, Faculty of Medical Sciences, University of Fukui, Fukui, JapanSecond Department of Internal Medicine, Faculty of Medical Sciences, University of Fukui, Fukui, JapanSecond Department of Internal Medicine, Faculty of Medical Sciences, University of Fukui, Fukui, JapanDepartment of Neurology, Fujita Neurological Hospital, Fukui, JapanDepartment of Pharmacology, Faculty of Medical Sciences, University of Fukui, Fukui, JapanDepartment of Molecular Pathology, Faculty of Medical Sciences, University of Fukui, Fukui, JapanBrain Bank for Aging Research, Tokyo Metropolitan Institute for Geriatrics and Gerontology, Tokyo, JapanBrain Bank for Aging Research, Tokyo Metropolitan Institute for Geriatrics and Gerontology, Tokyo, JapanBrain Bank for Aging Research, Tokyo Metropolitan Institute for Geriatrics and Gerontology, Tokyo, JapanSecond Department of Internal Medicine, Faculty of Medical Sciences, University of Fukui, Fukui, JapanSpleen tyrosine kinase (Syk), a non-receptor-type tyrosine kinase, has a wide range of physiological functions. A possible role of Syk in Alzheimer's disease (AD) has been proposed. We evaluated the localization of Syk in the brains of patients with AD and control participants. Human neuroblastoma M1C cells harboring wild-type tau (4R0N) were used with the tetracycline off (TetOff) induction system. In this model of neuronal tauopathy, the effects of the Syk inhibitors—BAY 61–3606 and R406—on tau phosphorylation and oligomerization were explored using several phosphorylated tau-specific antibodies and an oligomeric tau antibody, and the effects of these Syk inhibitors on autophagy were examined using western blot analyses. Moreover, the effects of the Syk inhibitor R406 were evaluated in vivo using wild-type mice. In AD brains, Syk and phosphorylated tau colocalized in the cytosol. In M1C cells, Syk protein (72 kDa) was detected using western blot analysis. Syk inhibitors decreased the expression levels of several tau phosphoepitopes including PHF-1, CP13, AT180, and AT270. Syk inhibitors also decreased the levels of caspase-cleaved tau (TauC3), a pathological tau form. Syk inhibitors increased inactivated glycogen synthase kinase 3β expression and decreased active p38 mitogen-activated protein kinase expression and demethylated protein phosphatase 2 A levels, indicating that Syk inhibitors inactivate tau kinases and activate tau phosphatases. Syk inhibitors also activated autophagy, as indicated by increased LC3II and decreased p62 levels. In vivo, the Syk inhibitor R406 decreased phosphorylated tau levels in wild-type mice. These findings suggest that Syk inhibitors offer novel therapeutic strategies for tauopathies, including AD.http://www.sciencedirect.com/science/article/pii/S0969996124002560Alzheimer's diseaseSykTauPhosphorylationAutophagyCaspase 3
spellingShingle Tomohisa Yamaguchi
Tadanori Hamano
Kiyonao Sada
Rei Asano
Nicholas M. Kanaan
Hirohito Sasaki
Shu-Hui Yen
Yuki Kitazaki
Yoshinori Endo
Soichi Enomoto
Norimichi Shirafuji
Masamichi Ikawa
Osamu Yamamura
Youshi Fujita
Koji Aoki
Hironobu Naiki
Maho Morishima
Yuko Saito
Shigeo Murayama
Yasunari Nakamoto
Syk inhibitors reduce tau protein phosphorylation and oligomerization
Neurobiology of Disease
Alzheimer's disease
Syk
Tau
Phosphorylation
Autophagy
Caspase 3
title Syk inhibitors reduce tau protein phosphorylation and oligomerization
title_full Syk inhibitors reduce tau protein phosphorylation and oligomerization
title_fullStr Syk inhibitors reduce tau protein phosphorylation and oligomerization
title_full_unstemmed Syk inhibitors reduce tau protein phosphorylation and oligomerization
title_short Syk inhibitors reduce tau protein phosphorylation and oligomerization
title_sort syk inhibitors reduce tau protein phosphorylation and oligomerization
topic Alzheimer's disease
Syk
Tau
Phosphorylation
Autophagy
Caspase 3
url http://www.sciencedirect.com/science/article/pii/S0969996124002560
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