Please use this identifier to cite or link to this item:
http://hdl.handle.net/2445/103642
Title: | MiniAp-4: A Venom-Inspired Peptidomimetic for Brain Delivery |
Author: | Oller Salvia, Benjamí Sánchez Navarro, Macarena Ciudad Fernández, 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 Venom 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. |
Note: | Reproducció del document publicat a: https://doi.org/10.1002/anie.201508445 |
It is part of: | Angewandte Chemie International Edition, 2016, vol. 55, num. 2, p. 572-575 |
URI: | http://hdl.handle.net/2445/103642 |
Related resource: | https://doi.org/10.1002/anie.201508445 |
ISSN: | 0003-3022 |
Appears in Collections: | Articles publicats en revistes (Química Inorgànica i Orgànica) Articles publicats en revistes (Institut de Recerca Biomèdica (IRB Barcelona)) |
Files in This Item:
File | Description | Size | Format | |
---|---|---|---|---|
657016.pdf | 2.84 MB | Adobe PDF | View/Open |
This item is licensed under a Creative Commons License