Identification of β-aminopyrrolidine containing peptides as β-amyloid aggregation inhibitors for Alzheimer's disease.

Alzheimer's disease (AD) is caused by a series of events initiated by the production and aggregation of the amyloid β-protein (Aβ). In the early stages of the disease, Aβ is released in a soluble form then progressively forms oligomeric, multimeric, and fibrillar aggregates, triggering neurodegeneration. Thus, development of inhibitors that initiate reverse Aβ aggregation is thought to be a logical approach in treating AD. In this context, we developed β-aminopyrrolidine containing 12 mer peptide 3 which is very potent in inhibiting the Aβ aggregation and also reducing Aβ(42)-induced cytotoxicity.