Related Experiment Video
Updated: May 15, 2026

Selection of Aptamers for Amyloid β-Protein, the Causative Agent of Alzheimer's Disease
Published on: May 13, 2010
Bivalent ligands targeting multiple pathological factors involved in Alzheimer's disease
Kai Liu1, Ronak Gandhi, Jiangmin Chen
1Department of Medicinal Chemistry, Virginia Commonwealth University, Richmond, Virginia, USA.
Abstract:
In a continuing effort to develop multifunctional compounds as potential treatment agents for Alzheimer's disease (AD), a series of bivalent ligands containing curcumin and cholesterylamine were designed, synthesized, and biologically characterized. Biological characterization supported earlier results that the spacer length and its attachment position on curcumin are essential structural determinants for biological activity in this class. Compounds with a spacer length of 17 to 21 atoms exhibited optimal neuroprotection in human neuroblastoma MC65 cells with submicromolar potency. These compounds inhibited the formation of amyloid-β oligomers (AβOs) and exhibited antioxidative activities in MC65 cells. Bivalent ligand 8, with its spacer (length of 17 atoms) connected at the methylene carbon between the two carbonyls of curcumin moiety is the most potent with an EC(50) of 0.083 ± 0.017 μM. In addition, 8 formed complex with biometals, such as Cu, Fe and Zn. Collectively, the results strongly support our assertion that these compounds are designed bivalent ligands with potential as multifunctional and neuroprotective agents.
Related Concept Videos
Ligand-Gated Ion Channel Receptor: Gating Mechanism
Ligand-gated Ion Channels
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that include the...
Alzheimer's Disease: Treatment
Alzheimer Disease ll: Pathophysiology
Alzheimer's Disease: Overview
The clinical diagnosis of AD hinges on the presence of memory and other cognitive impairments. Biomarkers, such as changes in Aβ and tau...
Alzheimer Disease l: Introduction