Applying the retro-enantio approach to obtain a peptide capable of overcoming the blood-brain barrier

Roger Prades; Benjamí Oller-Salvia; Susanne M. Schwarzmaier; Javier Selva; María Moros; Matilde Balbi; Valeria Grazú; Jesus M. De La Fuente; Gustavo Egea; Nikolaus Plesnila; Meritxell Teixidõ; Ernest Giralt

doi:10.1002/anie.201411408

Applying the retro-enantio approach to obtain a peptide capable of overcoming the blood-brain barrier

Roger Prades, Benjamí Oller-Salvia, Susanne M. Schwarzmaier, Javier Selva, María Moros, Matilde Balbi, Valeria Grazú, Jesus M. De La Fuente, Gustavo Egea, Nikolaus Plesnila, Meritxell Teixidõ, Ernest Giralt

Research output: Indexed journal article › Article › peer-review

103 Citations (Scopus)

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.

Original language	English
Pages (from-to)	3967-3972
Number of pages	6
Journal	Angewandte Chemie - International Edition
Volume	54
Issue number	13
DOIs	https://doi.org/10.1002/anie.201411408
Publication status	Published - 23 Mar 2015
Externally published	Yes

Keywords

blood-brain barrier
enantioselectivity
membranes
peptides
receptors

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10.1002/anie.201411408

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Prades, R., Oller-Salvia, B., Schwarzmaier, S. M., Selva, J., Moros, M., Balbi, M., Grazú, V., De La Fuente, J. M., Egea, G., Plesnila, N., Teixidõ, M., & Giralt, E. (2015). Applying the retro-enantio approach to obtain a peptide capable of overcoming the blood-brain barrier. Angewandte Chemie - International Edition, 54(13), 3967-3972. https://doi.org/10.1002/anie.201411408

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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.",

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Prades, R, Oller-Salvia, B, Schwarzmaier, SM, Selva, J, Moros, M, Balbi, M, Grazú, V, De La Fuente, JM, Egea, G, Plesnila, N, Teixidõ, M & Giralt, E 2015, 'Applying the retro-enantio approach to obtain a peptide capable of overcoming the blood-brain barrier', Angewandte Chemie - International Edition, vol. 54, no. 13, pp. 3967-3972. https://doi.org/10.1002/anie.201411408

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AU - Prades, Roger

AU - Oller-Salvia, Benjamí

AU - Schwarzmaier, Susanne M.

AU - Selva, Javier

AU - Moros, María

AU - Balbi, Matilde

AU - Grazú, Valeria

AU - De La Fuente, Jesus M.

AU - Egea, Gustavo

AU - Plesnila, Nikolaus

AU - Teixidõ, Meritxell

AU - Giralt, Ernest

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KW - enantioselectivity

KW - membranes

KW - peptides

KW - receptors

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JO - Angewandte Chemie - International Edition

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IS - 13

ER -

Applying the retro-enantio approach to obtain a peptide capable of overcoming the blood-brain barrier

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Keywords

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