Small molecule, non-peptide p75 ligands inhibit Abeta-induced neurodegeneration and synaptic impairment.

The p75 neurotrophin receptor (p75(NTR)) is expressed by neurons particularly vulnerable in Alzheimer's disease (AD). We tested the hypothesis that non-peptide, small molecule p75(NTR) ligands found to promote survival signaling might prevent Abeta-induced degeneration and synaptic dysfunction....

Full description

Saved in:
Bibliographic Details
Main Authors: Tao Yang, Juliet K Knowles, Qun Lu, Hong Zhang, Ottavio Arancio, Laura A Moore, Timothy Chang, Qian Wang, Katrin Andreasson, Jayakumar Rajadas, Gerald G Fuller, Youmei Xie, Stephen M Massa, Frank M Longo
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2008-01-01
Series:PLoS ONE
Online Access:https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0003604&type=printable
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1850240521328394240
author Tao Yang
Juliet K Knowles
Qun Lu
Hong Zhang
Ottavio Arancio
Laura A Moore
Timothy Chang
Qian Wang
Katrin Andreasson
Jayakumar Rajadas
Gerald G Fuller
Youmei Xie
Stephen M Massa
Frank M Longo
author_facet Tao Yang
Juliet K Knowles
Qun Lu
Hong Zhang
Ottavio Arancio
Laura A Moore
Timothy Chang
Qian Wang
Katrin Andreasson
Jayakumar Rajadas
Gerald G Fuller
Youmei Xie
Stephen M Massa
Frank M Longo
author_sort Tao Yang
collection DOAJ
description The p75 neurotrophin receptor (p75(NTR)) is expressed by neurons particularly vulnerable in Alzheimer's disease (AD). We tested the hypothesis that non-peptide, small molecule p75(NTR) ligands found to promote survival signaling might prevent Abeta-induced degeneration and synaptic dysfunction. These ligands inhibited Abeta-induced neuritic dystrophy, death of cultured neurons and Abeta-induced death of pyramidal neurons in hippocampal slice cultures. Moreover, ligands inhibited Abeta-induced activation of molecules involved in AD pathology including calpain/cdk5, GSK3beta and c-Jun, and tau phosphorylation, and prevented Abeta-induced inactivation of AKT and CREB. Finally, a p75(NTR) ligand blocked Abeta-induced hippocampal LTP impairment. These studies support an extensive intersection between p75(NTR) signaling and Abeta pathogenic mechanisms, and introduce a class of specific small molecule ligands with the unique ability to block multiple fundamental AD-related signaling pathways, reverse synaptic impairment and inhibit Abeta-induced neuronal dystrophy and death.
format Article
id doaj-art-94a2899ce30f40dcafdb4ae05c1625d0
institution OA Journals
issn 1932-6203
language English
publishDate 2008-01-01
publisher Public Library of Science (PLoS)
record_format Article
series PLoS ONE
spelling doaj-art-94a2899ce30f40dcafdb4ae05c1625d02025-08-20T02:00:51ZengPublic Library of Science (PLoS)PLoS ONE1932-62032008-01-01311e360410.1371/journal.pone.0003604Small molecule, non-peptide p75 ligands inhibit Abeta-induced neurodegeneration and synaptic impairment.Tao YangJuliet K KnowlesQun LuHong ZhangOttavio ArancioLaura A MooreTimothy ChangQian WangKatrin AndreassonJayakumar RajadasGerald G FullerYoumei XieStephen M MassaFrank M LongoThe p75 neurotrophin receptor (p75(NTR)) is expressed by neurons particularly vulnerable in Alzheimer's disease (AD). We tested the hypothesis that non-peptide, small molecule p75(NTR) ligands found to promote survival signaling might prevent Abeta-induced degeneration and synaptic dysfunction. These ligands inhibited Abeta-induced neuritic dystrophy, death of cultured neurons and Abeta-induced death of pyramidal neurons in hippocampal slice cultures. Moreover, ligands inhibited Abeta-induced activation of molecules involved in AD pathology including calpain/cdk5, GSK3beta and c-Jun, and tau phosphorylation, and prevented Abeta-induced inactivation of AKT and CREB. Finally, a p75(NTR) ligand blocked Abeta-induced hippocampal LTP impairment. These studies support an extensive intersection between p75(NTR) signaling and Abeta pathogenic mechanisms, and introduce a class of specific small molecule ligands with the unique ability to block multiple fundamental AD-related signaling pathways, reverse synaptic impairment and inhibit Abeta-induced neuronal dystrophy and death.https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0003604&type=printable
spellingShingle Tao Yang
Juliet K Knowles
Qun Lu
Hong Zhang
Ottavio Arancio
Laura A Moore
Timothy Chang
Qian Wang
Katrin Andreasson
Jayakumar Rajadas
Gerald G Fuller
Youmei Xie
Stephen M Massa
Frank M Longo
Small molecule, non-peptide p75 ligands inhibit Abeta-induced neurodegeneration and synaptic impairment.
PLoS ONE
title Small molecule, non-peptide p75 ligands inhibit Abeta-induced neurodegeneration and synaptic impairment.
title_full Small molecule, non-peptide p75 ligands inhibit Abeta-induced neurodegeneration and synaptic impairment.
title_fullStr Small molecule, non-peptide p75 ligands inhibit Abeta-induced neurodegeneration and synaptic impairment.
title_full_unstemmed Small molecule, non-peptide p75 ligands inhibit Abeta-induced neurodegeneration and synaptic impairment.
title_short Small molecule, non-peptide p75 ligands inhibit Abeta-induced neurodegeneration and synaptic impairment.
title_sort small molecule non peptide p75 ligands inhibit abeta induced neurodegeneration and synaptic impairment
url https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0003604&type=printable
work_keys_str_mv AT taoyang smallmoleculenonpeptidep75ligandsinhibitabetainducedneurodegenerationandsynapticimpairment
AT julietkknowles smallmoleculenonpeptidep75ligandsinhibitabetainducedneurodegenerationandsynapticimpairment
AT qunlu smallmoleculenonpeptidep75ligandsinhibitabetainducedneurodegenerationandsynapticimpairment
AT hongzhang smallmoleculenonpeptidep75ligandsinhibitabetainducedneurodegenerationandsynapticimpairment
AT ottavioarancio smallmoleculenonpeptidep75ligandsinhibitabetainducedneurodegenerationandsynapticimpairment
AT lauraamoore smallmoleculenonpeptidep75ligandsinhibitabetainducedneurodegenerationandsynapticimpairment
AT timothychang smallmoleculenonpeptidep75ligandsinhibitabetainducedneurodegenerationandsynapticimpairment
AT qianwang smallmoleculenonpeptidep75ligandsinhibitabetainducedneurodegenerationandsynapticimpairment
AT katrinandreasson smallmoleculenonpeptidep75ligandsinhibitabetainducedneurodegenerationandsynapticimpairment
AT jayakumarrajadas smallmoleculenonpeptidep75ligandsinhibitabetainducedneurodegenerationandsynapticimpairment
AT geraldgfuller smallmoleculenonpeptidep75ligandsinhibitabetainducedneurodegenerationandsynapticimpairment
AT youmeixie smallmoleculenonpeptidep75ligandsinhibitabetainducedneurodegenerationandsynapticimpairment
AT stephenmmassa smallmoleculenonpeptidep75ligandsinhibitabetainducedneurodegenerationandsynapticimpairment
AT frankmlongo smallmoleculenonpeptidep75ligandsinhibitabetainducedneurodegenerationandsynapticimpairment