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

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Resum

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.

Idioma original	Anglès
Pàgines (de-a)	3967-3972
Nombre de pàgines	6
Revista	Angewandte Chemie - International Edition
Volum	54
Número	13
DOIs	https://doi.org/10.1002/anie.201411408
Estat de la publicació	Publicada - 23 de març 2015
Publicat externament	Sí

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

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",

author = "Roger Prades and Benjam{\'i} Oller-Salvia and Schwarzmaier, \{Susanne M.\} and Javier Selva and Mar{\'i}a Moros and Matilde Balbi and Valeria Graz{\'u} and \{De La Fuente\}, \{Jesus M.\} and Gustavo Egea and Nikolaus Plesnila and Meritxell Teixid{\~o} and Ernest Giralt",

note = "Publisher Copyright: {\textcopyright} 2015 WILEY-VCH Verlag GmbH \& Co. KGaA, Weinheim.",

year = "2015",

month = mar,

day = "23",

doi = "10.1002/anie.201411408",

language = "English",

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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, núm. 13, pàg. 3967-3972. https://doi.org/10.1002/anie.201411408

TY - JOUR

T1 - Applying the retro-enantio approach to obtain a peptide capable of overcoming the blood-brain barrier

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

PY - 2015/3/23

Y1 - 2015/3/23

N2 - 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.

AB - 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.

KW - blood-brain barrier

KW - enantioselectivity

KW - membranes

KW - peptides

KW - receptors

UR - https://www.scopus.com/pages/publications/84924869467

U2 - 10.1002/anie.201411408

DO - 10.1002/anie.201411408

M3 - Article

C2 - 25650865

AN - SCOPUS:84924869467

SN - 1433-7851

VL - 54

SP - 3967

EP - 3972

JO - Angewandte Chemie - International Edition

JF - Angewandte Chemie - International Edition

IS - 13

ER -

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

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