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Journal Articles Angewandte Chemie International Edition Year : 2016

MiniAp-4: A Venom-Inspired Peptidomimetic for Brain Delivery


Drug delivery across the blood-brain barrier (BBB) is a formidable challenge for therapies targeting the central nervous system. Although BBB shuttle peptides enhance transport into the brain non-invasively, their application is partly limited by lability to proteases. The present study proposes the use of cyclic peptides derived from venoms as an affordable way to circumvent this drawback. Apamin, a neurotoxin from bee venom, was minimized by reducing its complexity, toxicity, and immunogenicity, while preserving brain targeting, active transport, and protease resistance. Among the analogues designed, the monocyclic lactam-bridged peptidomimetic MiniAp-4 was the most permeable. This molecule is capable of translocating proteins and nanoparticles in a human-cell-based BBB model. Furthermore, MiniAp-4 can efficiently deliver a cargo across the BBB into the brain parenchyma of mice.

Dates and versions

hal-02513287 , version 1 (20-03-2020)



Benjamí Oller-Salvia, Macarena Sánchez-Navarro, Sonia Ciudad, Marc Guiu, Pol Arranz-Gibert, et al.. MiniAp-4: A Venom-Inspired Peptidomimetic for Brain Delivery. Angewandte Chemie International Edition, 2016, 55 (2), pp.572-575. ⟨10.1002/anie.201508445⟩. ⟨hal-02513287⟩


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