Current Bioactive Compounds

Adriano Mollica
Department of Pharmacy, University ”G. d' Annunzio” of Chieti-Pescara
Via dei Vestini 31
Chieti, 66100
Italy

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Structural Features of Small Molecule Amyloid-Beta Self-Assembly Inhibitors

Author(s): Bela Torok, Seema Bag, Madhura Sarkar, Sujaya Dasgupta, Marianna Torok.

Abstract:

The role of various structural features, namely basic scaffolds and substituents of small molecule inhibitors of the self-assembly of amyloid-beta (Aβ) peptide, a key process in Alzheimer’s disease, is described. The literature analysis in this update extends to the past 5 years, thus the past 15 year period is covered. In addition, while our previous review was limited to anti-fibril agents the current update includes compounds with a major profile in oligomer inhibition as well, and covers inhibitors of the broadly defined Aβ self-assembly. Basis sets of 507 fibrillogenesis inhibitors and 154 oligomer formation inhibitors were surveyed and a chemical map of the inhibitors is provided highlighting the most common substituents that appear in these compounds.

Keywords: Alzheimer’s disease, amyloid, amyloid-beta peptide, self-assembly, fibrils, oligomers, small molecule inhibitors, structure-activity relationship

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Article Details

VOLUME: 9
ISSUE: 1
Year: 2013
Page: [37 - 63]
Pages: 27
DOI: 10.2174/1573407211309010006