Journal
TETRAHEDRON LETTERS
Volume 56, Issue 23, Pages 3670-3673Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2015.02.132
Keywords
alpha-Helix mimetics; Amyloid beta-peptides; Diabetes; Helical structures; Proteomimetics
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The abnormal deposition of proteins as insoluble plaques is associated with many diseases, including Alzheimer's, Parkinson's and type II diabetes. There is an unmet need for synthetic agents that are able to mediate particular steps in the pathway between soluble proteins in their native unfolded state and their insoluble beta-sheet rich aggregates. We have previously reported classes of alpha-helix mimetic that agonize or antagonize islet amyloid polypeptide aggregation, depending on the presence of a lipid bilayer. Here we investigate a novel mixed benzamide and pyridylamide scaffold that gives improved activity and explores the role of side-chain polarity, backbone rigidity and curvature in inhibiting lipid-catalyzed fibrillization. (C) 2015 Published by Elsevier Ltd.
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