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Applying the Retro‐Enantio Approach To Obtain a Peptide Capable of Overcoming the Blood–Brain Barrier |
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| 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 |
| Affiliation: | 1. Institute for Research in Biomedicine, Baldiri Reixac 10, 08028 Barcelona (Spain);2. Department of Neurodegeneration, Royal College of Surgeons in Ireland (RCSI) (Ireland);3. Institute for Stroke and Dementia Research (ISD), Ludwig Maximilians University Munich (Germany);4. IDIBAPS, IN2UB, University of Barcelona (Spain);5. Instituto de Nanociencia de Aragon (INA) (Spain);6. Munich Cluster of Systems Neurology (Synergy), Munich (Germany);7. Department of Organic Chemistry, University of Barcelona (Spain) |
| 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. |
| Keywords: | blood– brain barrier enantioselectivity membranes peptides receptors |