ACS Chemical Neuroscience · 2011 · 86 citations · 24 references
Life SciencesMedicinal ChemistryPharmacologyDrug DiscoveryNeurodegenerationProdrug DesignAlzheimer DiseaseAmyloid FormationNanomedicineNatural Product Drug DiscoveryNeurodegenerative Disease PharmacologyProtein AggregationAmyloid Beta AggregationAmyloid Beta PeptidesAmyloid InhibitionInhibition Of Amyloid FormationPeptide AggregationProtein Aggregation InhibitorsTau AggregationTau Protein Aggregation
The synthesis of a water/plasma soluble, noncytotoxic, "clicked" sugar-derivative of curcumin with amplified bioefficacy in modulating amyloid-β and tau peptide aggregation is presented. Curcumin inhibits amyloid-β and tau peptide aggregation at micromolar concentrations; the sugar-curcumin conjugate inhibits Aβ and tau peptide aggregation at concentrations as low as 8 nM and 0.1 nM, respectively. In comparison to curcumin, this conveniently synthesized Alzheimer's drug candidate is a more powerful antioxidant.
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Common Structure of Soluble Amyloid Oligomers Implies Common Mechanism of Pathogenesis
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Medicine, Oncology, Pharmacology +10
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