Verteporfin is a substrate-selective γ-secretase inhibitor that binds the amyloid precursor protein transmembrane domain

Verteporfin is a substrate-selective γ-secretase inhibitor that binds the amyloid precursor protein transmembrane domain

This work reports substrate-selective inhibition of a protease with broad substrate specificity based on direct binding of a small-molecule inhibitor to the substrate. The target for these studies was γ-secretase protease, which cleaves dozens of different single-span membrane protein substrates, in...

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Bibliographic Details
Main Authors: Beg, I. (Author), Castro, M.A (Author), Levesque, I. (Author), Nurmakova, K. (Author), Parson, K.F (Author), Ruotolo, B.T (Author), Sanders, C.R (Author), Voehler, M.W (Author), Wilkinson, M.C (Author), Wolfe, M.S (Author)
Format: Article
Language:English
Published: American Society for Biochemistry and Molecular Biology Inc. 2022
Subjects:
Activation analysis
Amyloid precursor proteins
Binders
Direct bindings
Glycoproteins
Membrane proteins
Molecules
Proteins
Selective inhibition
Small molecules
Substrate specificity
Substrates
Transmembrane domain
Trans-membrane domains
γ-secretase
γ-secretase inhibitors
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