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Dissociation of haemolytic and oligomer-preventing activities of gramicidin S derivatives targeting the amyloid-β N-terminus

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Abstract

The intrinsic haemolysis of an amyloid-β (Aβ) N-terminal targeting gramicidin S derivative was successfully dissociated from its Aβ oligomer-preventing activities via Ala-scanning-based regulation of molecular amphiphilicity. The representative analogue DGR-7 shows low toxicity but significant efficiency in preventing Aβ oligomers and reducing amyloid plaques in APP/PS1 transgenic AD mice.

Graphical abstract: Dissociation of haemolytic and oligomer-preventing activities of gramicidin S derivatives targeting the amyloid-β N-terminus

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Publication details

The article was received on 23 Oct 2017, accepted on 24 Nov 2017 and first published on 30 Nov 2017


Article type: Communication
DOI: 10.1039/C7CC08180D
Citation: Chem. Commun., 2017, Advance Article
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    Dissociation of haemolytic and oligomer-preventing activities of gramicidin S derivatives targeting the amyloid-β N-terminus

    D. Chen, W. Qin, G. Wen, B. Shi, Z. Liu, Y. Wang, Q. Zhou, J. Quan, B. Zhou and X. Bu, Chem. Commun., 2017, Advance Article , DOI: 10.1039/C7CC08180D

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