Issue 41, 2012
From the journal:

Organic & Biomolecular Chemistry

Optimisation of BACE1 inhibition of tripartite structures by modification of membrane anchors, spacers and pharmacophores – development of potential agents for the treatment of Alzheimer's disease†

Philipp Linning,a   Ute Haussmann,b   Isaak Beyer,a   Sebastian Weidlich,a   Heinke Schieb,b   Jens Wiltfang,b   Hans-Wolfgang Klafki*b  and  Hans-Joachim Knölker*a  

* Corresponding authors

a Department Chemie, Technische Universität Dresden, Bergstrasse 66, 01069 Dresden, Germany
E-mail: hans-joachim.knoelker@tu-dresden.de

b LVR Klinikum Essen, Klinik für Psychiatrie und Psychotherapie, Universität Duisburg-Essen, Virchowstrasse 171, 45147 Essen, Germany
E-mail: hans.klafki@uni-due.de

Abstract

Systematic variation of membrane anchor, spacer and pharmacophore building blocks leads to an optimisation of the inhibitory effect of tripartite structures towards BACE1-induced cleavage of the amyloid precursor protein (APP).

Graphical abstract: Optimisation of BACE1 inhibition of tripartite structures by modification of membrane anchors, spacers and pharmacophores – development of potential agents for the treatment of Alzheimer's disease

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Article information

DOI
https://doi.org/10.1039/C2OB26103K
Article type
Paper
Submitted
07 Jun 2012
Accepted
02 Aug 2012
First published
03 Aug 2012

Org. Biomol. Chem., 2012,10, 8216-8235

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Optimisation of BACE1 inhibition of tripartite structures by modification of membrane anchors, spacers and pharmacophores – development of potential agents for the treatment of Alzheimer's disease

P. Linning, U. Haussmann, I. Beyer, S. Weidlich, H. Schieb, J. Wiltfang, H. Klafki and H. Knölker, Org. Biomol. Chem., 2012, 10, 8216 DOI: 10.1039/C2OB26103K

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