Abstract
The role of the chemical structure, namely the effect of substituents, of small molecule inhibitors in selfassembly of Alzheimers disease related amyloid-beta peptide is discussed. The literature analysis is concentrated on the past 10 years and analyzed the structure of Aβ inhibitors pointing out common features. A basis set of 321 compounds is reviewed and a chemical map of the inhibitors is provided highlighting the most common substituents that appear in these molecules. Based on the findings, aromatic/heteroaromatic groups were found to be present in an overwhelming majority of inhibitors (95%). Acidic substituents appeared the second most common substituent group (67%) suggesting the importance of these motifs as possible binding units. Several structure activity relationship studies that support this role are also discussed.
Keywords: Alzheimer's disease, amyloid, amyloid-beta peptide, self-assembly, fibrillogenesis, small molecule inhibitors, structure-activity relationship
Current Bioactive Compounds
Title: Chemistry of Small Molecule Inhibitors in Self-Assembly of Alzheimers Disease Related Amyloid-Beta Peptide
Volume: 4 Issue: 3
Author(s): Bela Torok, Sujaya Dasgupta and Marianna Torok
Affiliation:
Keywords: Alzheimer's disease, amyloid, amyloid-beta peptide, self-assembly, fibrillogenesis, small molecule inhibitors, structure-activity relationship
Abstract: The role of the chemical structure, namely the effect of substituents, of small molecule inhibitors in selfassembly of Alzheimers disease related amyloid-beta peptide is discussed. The literature analysis is concentrated on the past 10 years and analyzed the structure of Aβ inhibitors pointing out common features. A basis set of 321 compounds is reviewed and a chemical map of the inhibitors is provided highlighting the most common substituents that appear in these molecules. Based on the findings, aromatic/heteroaromatic groups were found to be present in an overwhelming majority of inhibitors (95%). Acidic substituents appeared the second most common substituent group (67%) suggesting the importance of these motifs as possible binding units. Several structure activity relationship studies that support this role are also discussed.
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Cite this article as:
Torok Bela, Dasgupta Sujaya and Torok Marianna, Chemistry of Small Molecule Inhibitors in Self-Assembly of Alzheimers Disease Related Amyloid-Beta Peptide, Current Bioactive Compounds 2008; 4 (3) . https://dx.doi.org/10.2174/157340708786305970
DOI https://dx.doi.org/10.2174/157340708786305970 |
Print ISSN 1573-4072 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6646 |
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