Optimization 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

Authors: Linning, Philipp; Haussmann, Ute; Beyer, Isaak; Weidlich, Sebastian; Schieb, Heinke; Wiltfang, Jens; Klafki, Hans-Wolfgang; Knoelker, Hans-Joachim; Organic & Biomolecular Chemistry; (2012); 10.1039/c2ob26103k

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).