Beta-sheet breakers for Alzheimer's disease therapy

• Published in: Current drug targets Vol. 5; no. 6; p. 553
• Main Authors: Bieler, S, Soto, C
• Format: Journal Article
• Language: English
• Published: United Arab Emirates 01.08.2004
• Subjects: Alzheimer Disease - drug therapy; Alzheimer Disease - genetics; Alzheimer Disease - metabolism; Amyloid beta-Peptides - adverse effects; Amyloid beta-Peptides - antagonists & inhibitors; Amyloid beta-Peptides - metabolism; Amyloid beta-Protein Precursor - adverse effects; Amyloid beta-Protein Precursor - genetics; Amyloid beta-Protein Precursor - metabolism; Animals; Gene Expression - genetics; Humans; Models, Biological; Peptide Fragments - adverse effects; Peptide Fragments - antagonists & inhibitors; Peptide Fragments - metabolism; Peptide Fragments - therapeutic use
• ISSN: 1389-4501
• DOI: 10.2174/1389450043345290

A growing wealth of evidence indicates that the key pathological event in Alzheimer's disease is the conversion of the normal soluble amyloid-beta peptide into beta-sheet-rich oligomeric structures which have a neurotoxic activity and ability to form insoluble amyloid deposits that accumulate in the brain. Beta-sheet breakers constitute a new class of drugs that are designed to specifically bind amyloid-beta peptide and block and/or reverse this abnormal conformational change. In this article we review this approach, describe diverse compounds reported to have this activity and summarize the data supporting the view that beta-sheet breakers could be serious candidates to combat this devastating disease.