Article

Structural Analysis of Simultaneous Activation and Inhibition of γ-Secretase Activity in Development of Drugs for Alzheimer’s disease

2020-09-22

Abstract excerpt

<h4>Significance</h4> The majority of drugs that target membrane-embedded protease γ-secretase show unusual biphasic activation-inhibition dose-response in cells, model animals, and humans. Semagacestat and avagacestat are two biphasic-drugs that can facilitate cognitive decline in patients with Alzheimer’s disease. Initial mechanistic studies showed that the biphasic-drugs, and pathogenic mutations, can produce...

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Literature Corpus work: 8eabf53d-cea2-5ed1-bc30-7a3d1b947ba6
DOI: 10.1101/2020.09.22.307959

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