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Identification of a small molecule beta-secretase inhibitor that binds without catalytic aspartate engagement.
Steele, Thomas G; Hills, Ivory D; Nomland, Ashley A; de León, Pablo; Allison, Timothy; McGaughey, Georgia; Colussi, Dennis; Tugusheva, Katherine; Haugabook, Sharie J; Espeseth, Amy S; Zuck, Paul; Graham, Samuel L; Stachel, Shawn J.
  • Steele TG; Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co, West Point, PA 19486, USA.
Bioorg Med Chem Lett ; 19(1): 17-20, 2009 Jan 01.
Article en En | MEDLINE | ID: mdl-19036583
ABSTRACT
A small molecule inhibitor of beta-secretase with a unique binding mode has been developed. Crystallographic determination of the enzyme-inhibitor complex shows the catalytic aspartate residues in the active site are not engaged in inhibitor binding. This unprecedented binding mode in the field of aspartyl protease inhibition is described.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Ácido Aspártico / Inhibidores Enzimáticos / Secretasas de la Proteína Precursora del Amiloide Tipo de estudio: Diagnostic_studies Idioma: En Año: 2009 Tipo del documento: Article
Texto completo
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Search on Google

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Ácido Aspártico / Inhibidores Enzimáticos / Secretasas de la Proteína Precursora del Amiloide Tipo de estudio: Diagnostic_studies Idioma: En Año: 2009 Tipo del documento: Article