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Fragment Binding to β-Secretase 1 without Catalytic Aspartate Interactions Identified via Orthogonal Screening Approaches

[Image: see text] An approach to identify β-secretase 1 (BACE1) fragment binders that do not interact with the catalytic aspartate dyad is presented. A ThermoFluor (thermal shift) and a fluorescence resonance energy transfer enzymatic screen on the soluble domain of BACE1, together with a surface pl...

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Detalles Bibliográficos
Autores principales: Rombouts, Frederik J. R., Alexander, Richard, Cleiren, Erna, De Groot, Alex, Carpentier, Michel, Dijkmans, Joyce, Fierens, Katleen, Masure, Stefan, Moechars, Diederik, Palomino-Schätzlein, Martina, Pineda-Lucena, Antonio, Trabanco, Andrés A., Van Glabbeek, Daan, Vos, Ann, Tresadern, Gary
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2017
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5472370/
https://www.ncbi.nlm.nih.gov/pubmed/28626832
http://dx.doi.org/10.1021/acsomega.6b00482