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Title: MiniAp-4: A Venom-Inspired Peptidomimetic for Brain Delivery
Author: Oller Salvia, Benjamí
Sánchez Navarro, Macarena
Ciudad, Sonia
Guiu, Marc
Arranz Gibert, Pol
García, Cristina
Gomis i Cabré, Roger
Cecchelli, Roméo
García Arroyo, Jesús
Giralt Lledó, Ernest
Teixidó Turà, Meritxell
Keywords: Verins animals
Síntesi de pèptids
Malalties cerebrals
Peptide synthesis
Brain diseases
Issue Date: 5-Jan-2016
Publisher: Wiley
Abstract: 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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It is part of: Angewandte Chemie International Edition, 2016, vol. 55, num. 2, p. 572-575
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ISSN: 0003-3022
Appears in Collections:Articles publicats en revistes (Institut de Recerca Biomèdica (IRB Barcelona))
Articles publicats en revistes (Química Inorgànica i Orgànica)

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