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

Daoyuan Chen; Wenjing Qin; Gesi Wen; Bihua Shi; Ziyi Liu; Youqiao Wang; Qiang Zhou; Junmin Quan; Binhua Zhou; Xianzhang Bu

doi:10.1039/C7CC08180D

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

Daoyuan Chen,^a Wenjing Qin,^a Gesi Wen,^a Bihua Shi,^b Ziyi Liu,^a Youqiao Wang,^a Qiang Zhou,^b Junmin Quan,^b Binhua Zhou

*^a and Xianzhang Bu

*^a

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* Corresponding authors

^a School of Pharmaceutical Sciences, Sun Yat-sen University, GuangZhou 510006, China
E-mail: zhoubh5@mail.sysu.edu.cn, phsbxzh@mail.sysu.edu.cn

^b Laboratory of Chemical Genomics, School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen 518055, China

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.

Chemical Communications

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

Abstract

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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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