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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†
Philipp Linning,Ute Haussmann,Isaak Beyer,Sebastian Weidlich,Heinke Schieb,Jens Wiltfang,Hans-Wolfgang Klafki,Hans-Joachim Knölker
Organic & Biomolecular Chemistry Pub Date : 08/03/2012 00:00:00 , DOI:10.1039/C2OB26103K
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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