Issue 19, 2009
From the journal:

Organic & Biomolecular Chemistry

A gorge-spanning, high-affinity cholinesterase inhibitor to explore β-amyloid plaques†

Paul W. Elsinghorst,a   Wolfgang Härtig,b   Simone Goldhammer,b   Jens Groschebc  and  Michael Gütschow*a  

* Corresponding authors

a Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, Bonn, Germany
E-mail: guetschow@uni-bonn.de
Fax: +49 228 732567
Tel: +49 228 732317

b Paul Flechsig Institute for Brain Research, Department for Neurophysiology, University of Leipzig, Jahnallee 59, Leipzig, Germany

c Interdisciplinary Center of Clinical Research (IZKF), Faculty of Medicine, University of Leipzig, Inselstraße 22, Leipzig, Germany

Abstract

Cholinesterases are involved in the pathological formation of β-amyloid plaques. To investigate this pathohistological hallmark of Alzheimer's disease we prepared a high-affinity, fluorescent cholinesterase inhibitor. Its fluorescence intensity was significantly enhanced upon binding to cholinesterases. Using this probe, brain samples from mice and humans affected by Alzheimer's disease were successfully analyzed for β-amyloid plaques. Unexpectedly, it was discovered, by competition experiments, that the compound binds to amyloid structures, rather than to cholinesterases inside of the plaques.

Graphical abstract: A gorge-spanning, high-affinity cholinesterase inhibitor to explore β-amyloid plaques

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Article information

DOI
https://doi.org/10.1039/B909612D
Article type
Paper
Submitted
14 May 2009
Accepted
16 Jun 2009
First published
17 Jul 2009

Org. Biomol. Chem., 2009,7, 3940-3946

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A gorge-spanning, high-affinity cholinesterase inhibitor to explore β-amyloid plaques

P. W. Elsinghorst, W. Härtig, S. Goldhammer, J. Grosche and M. Gütschow, Org. Biomol. Chem., 2009, 7, 3940 DOI: 10.1039/B909612D

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