Abstract
The interaction of amyloid beta peptide (Abeta) and Abeta-binding alcohol dehydrogenase (ABAD) was recently implicated in the pathogenesis of Alzheimer's disease (AD). Using an ELISA-based screening assay, we identified frentizole, an FDA-approved immunosuppressive drug, as a novel inhibitor of the Abeta-ABAD interaction. Analysis of the frentizole structure-activity relationship led to identification of a novel benzothiazole urea with a 30-fold improvement in potency.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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3-Hydroxyacyl CoA Dehydrogenases / metabolism*
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Amyloid beta-Peptides / metabolism*
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Benzothiazoles
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Enzyme-Linked Immunosorbent Assay
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Hydroxysteroid Dehydrogenases / metabolism*
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Inhibitory Concentration 50
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Molecular Structure
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Phenylurea Compounds / chemical synthesis
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Phenylurea Compounds / chemistry*
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Phenylurea Compounds / pharmacology*
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Protein Binding
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Structure-Activity Relationship
Substances
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Amyloid beta-Peptides
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Benzothiazoles
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Phenylurea Compounds
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frentizole
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Hydroxysteroid Dehydrogenases
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3-Hydroxyacyl CoA Dehydrogenases