Structure-based optimization of oxadiazole-based GSK-3 inhibitors

…, JM Dominguez, B Plotkin, H Eldar-Finkelman…

Index: Lo Monte, Fabio; Kramer, Thomas; Gu, Jiamin; Brodrecht, Martin; Pilakowski, Johannes; Fuertes, Ana; Dominguez, Juan Manuel; Plotkin, Batya; Eldar-Finkelman, Hagit; Schmidt, Boris European Journal of Medicinal Chemistry, 2013 , vol. 61, p. 26 - 40

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Citation Number: 19

Abstract

Inhibition of glycogen synthase kinase-3 (GSK-3) induces neuroprotective effects, eg decreases β-amyloid production and reduces tau hyperphosphorylation, which are both associated with Alzheimer's disease (AD). The two isoforms of GSK-3 in mammalians are GSK-3α and β, which share 98% homology in their catalytic domains. We investigated GSK- 3 inhibitors based on 2 different scaffolds in order to elucidate the demands of the ATP- ...