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

# metadata.dc.description.abstract[].value
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.

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Angewandte Chemie International Edition, 2016, vol. 55, num. 2, p. 572-575

# metadata.dc.rights[].value
cc-by-nc-nd (c) Oller Salvia, Benjamí et al., 2016

# metadata.dc.source[].value
Articles publicats en revistes (Química Inorgànica i Orgànica)

# metadata.dc.title[].value
MiniAp-4: A Venom-Inspired Peptidomimetic for Brain Delivery