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Article

Semagacestat Is a Pseudo-Inhibitor of γ-Secretase

1 Oct 2017

Abstract excerpt

γ-secretase inhibitors (GSI) are drugs developed to decrease amyloid-β peptide (Aβ) production by inhibiting intramembranous cleavage of β-amyloid protein precursor (βAPP). However, a large phase 3 trial of semagacestat, a potential non-transition state analog (non-TSA) GSI, in patients with Alzheimer's disease (AD) was terminated due to unexpected aggravation of cognitive deficits and side effects. Here, we show...

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PMID: 28978478
DOI: 10.1016/j.celrep.2017.09.032

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