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  4. Entacapone and tolcapone, two catechol O-methyltransferase inhibitors, block fibril formation of alpha-synuclein and beta-amyloid and protect against amyloid-induced toxicity
 
research article

Entacapone and tolcapone, two catechol O-methyltransferase inhibitors, block fibril formation of alpha-synuclein and beta-amyloid and protect against amyloid-induced toxicity

Di Giovanni, Saviana
•
Eleuteri, Simona
•
Paleologou, Katerina E.
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2010
Journal of Biological Chemistry

Parkinson disease (PD) is the second most common neurodegenerative disorder after Alzheimer disease (AD). There is considerable consensus that the increased production and/or aggregation of alpha-synuclein (alpha-syn) plays a central role in the pathogenesis of PD and related synucleinopathies. Current therapeutic strategies for treating PD offer mainly transient symptomatic relief and aim at the restitution of dopamine levels to counterbalance the loss of dopaminergic neurons. Therefore, the identification and development of drug-like molecules that block alpha-synuclein aggregation and prevent the loss of dopaminergic neurons are desperately needed to treat or slow the progression of PD. Here, we show that entacapone and tolcapone are potent inhibitors of alpha-syn and beta-amyloid (Abeta) oligomerization and fibrillogenesis, and they also protect against extracellular toxicity induced by the aggregation of both proteins. Comparison of the anti-aggregation properties of entacapone and tolcapone with the effect of five other catechol-containing compounds, dopamine, pyrogallol, gallic acid, caffeic acid, and quercetin on the oligomerization and fibrillization of alpha-syn and Abeta, demonstrate that the catechol moiety is essential for the anti-amyloidogenic activity. Our findings present the first characterization of the anti-amyloidogenic properties of tolcapone and entacapone against both alpha-synuclein and Abeta42 and highlight the potential of this class of nitro-catechol compounds as anti-amyloidogenic agents. Their inhibitory properties, mode of action, and structural properties suggest that they constitute promising lead compounds for further optimization.

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Type
research article
DOI
10.1074/jbc.M109.080390
Web of Science ID

WOS:000277399000015

Author(s)
Di Giovanni, Saviana
Eleuteri, Simona
Paleologou, Katerina E.
Yin, Guowei
Zweckstetter, Markus
Carrupt, Pierre-Alain
Lashuel, Hilal A.  
Date Issued

2010

Publisher

American Society for Biochemistry and Molecular Biology

Published in
Journal of Biological Chemistry
Volume

285

Issue

20

Start page

14941

End page

54

Editorial or Peer reviewed

NON-REVIEWED

Written at

EPFL

EPFL units
LMNN  
Available on Infoscience
November 2, 2009
Use this identifier to reference this record
https://infoscience.epfl.ch/handle/20.500.14299/44028
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