Applying the Retro-Enantio Approach To Obtain a Peptide Capable of Overcoming the Blood-Brain Barrier

被引：108

作者：

Prades, Roger ^{[1
]}

Oller-Salvia, Benjami ^{[1
]}

Schwarzmaier, Susanne M. ^{[2
,3
]}

Selva, Javier ^{[4
]}

Moros, Maria ^{[5
]}

Balbi, Matilde ^{[2
,3
]}

Grazu, Valeria ^{[5
]}

de la Fuente, Jesus M. ^{[5
]}

Egea, Gustavo ^{[4
]}

Plesnila, Nikolaus ^{[2
,3
,6
]}

Teixido, Meritxell ^{[1
]}

Giralt, Ernest ^{[1
]}

机构：

[1] Inst Res Biomed, Barcelona 08028, Spain

[2] Royal Coll Surgeons Ireland, Dept Neurodegenerat, Dublin 2, Ireland

[3] Univ Munich, Inst Stroke & Dementia Res ISD, Munich, Germany

[4] Univ Barcelona, IN2UB, IDIBAPS, E-08007 Barcelona, Spain

[5] INA, Barcelona, Spain

[6] Munich Cluster Syst Neurol SyNergy, Munich, Germany

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2015年 / 54卷 / 13期

关键词：

blood-brain barrier; enantioselectivity; membranes; peptides; receptors; TARGETED ABSOLUTE PROTEOMICS; IN-VITRO; DRUG-DELIVERY; TRANSFERRIN RECEPTOR; NANOPARTICLES; PERMEABILITY; TRANSPORTERS; MEMBRANE; PROTEINS; PROFILE;

D O I：

10.1002/anie.201411408

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

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.

引用

页码：3967 / 3972

页数：6

共 30 条

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[Anonymous], 2011, ANGEW CHEM, V123, P8148

[2]

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