Applying the Retro‐Enantio Approach to Obtain a Peptide Capable of Overcoming the Blood–Brain Barrier - Prades - 2015 - Angewandte Chemie International Edition - Wiley Online Library

Applying the Retro‐Enantio Approach to Obtain a Peptide Capable of Overcoming the Blood–Brain Barrier - Prades - 2015 - Angewandte Chemie International Edition - Wiley Online Library

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Applying the Retro-Enantio Approach to Obtain a Peptide Capable of Overcoming the Blood–Brain Barrier†

Authors

• Dr. Roger Prades,

• Benjamí Oller-Salvia,

• Dr. Susanne M. Schwarzmaier,

• Dr. Javier Selva,

• Dr. María Moros,

• Matilde Balbi,

• Dr. Valeria Grazú,

• Dr. Jesus M. de La Fuente,

• Prof. Gustavo Egea,

• Prof. Nikolaus Plesnila,

• Dr. Meritxell Teixidó,

• Prof. Ernest Giralt

• First published: 29 January 2015Full publication history
• DOI: 10.1002/anie.201411408View/save citation
• Cited by: 0 articles Check for new citations
• Funding Information

• † 
  We thank Dr. F. Hellal from the Institute for Stroke and Dementia Research (ISD), Ludwig Maximilians University and Dr. J. Colombelli from the Institute for Research in Biomedicine (IRB Barcelona) for their contribution and critical advice regarding the microscope images. We also thank Marc Guiu from the IRB Barcelona for his assistance in the IVIS in vivo imaging experiments. We thank an anonymous reviewer for drawing our attention to Ref. 22, the electronic version of which was published during the preparation of this manuscript. This study was supported by grants from ARAID, MINECO-FEDER (BIO2013-40716, BFU-2009-0786, and BFU-2012-33932), and the Generalitat de Catalunya (XRB and 2014-SGR-521). B.O.-S. is supported by a “La Caixa”/IRB Barcelona fellowship. We thank FARA, FEDAES/GENEFA, and the BABEL FAMILY for support.

Abstract

The blood–brain barrier (BBB) is a formidable physical and enzymatic barrier that tightly controls the passage of molecules from the blood to the brain. In fact, less than 2 % of all potential neurotherapeutics are able to cross it. Here, by applying the retro-enantio approach to a peptide that targets the transferrin receptor, a full protease-resistant peptide with the capacity to act as a BBB shuttle was obtained and thus enabled the transport of a variety of cargos into the central nervous system.