Uncovering the Binding Mode of γ -Secretase Inhibitors
نویسندگان
چکیده
منابع مشابه
The dynamic conformational landscape of γ-secretase
The structure and function of the gamma-secretase proteases are of great interest because of their crucial roles in cellular and disease processes. We established a novel purification protocol for the gamma-secretase complex that involves a conformation- and complex-specific nanobody, yielding highly pure and active enzyme. Using single particle electron microscopy, we analyzed the gamma-secret...
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γ-Secretase is an intramembrane-cleaving protease responsible for the generation of amyloid-β (Aβ) peptides. Recently, a series of compounds called γ-secretase modulators (GSMs) has been shown to decrease the levels of long toxic Aβ species (i.e., Aβ42), with a concomitant elevation of the production of shorter Aβ species. In this study, we show that a phenylimidazole-type GSM allosterically in...
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ژورنال
عنوان ژورنال: ACS Chemical Neuroscience
سال: 2019
ISSN: 1948-7193,1948-7193
DOI: 10.1021/acschemneuro.9b00272