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.
authors: Institute for Research in Biomedicine, Baldiri Reixac 10, 08028 Barcelona (Spain).
authors: Roger
authors: R
authors: Prades
authors: Benjamí
authors: B
authors: Oller-Salvia
authors: Susanne M
authors: SM
authors: Schwarzmaier
authors: Javier
authors: J
authors: Selva
authors: María
authors: M
authors: Moros
authors: Matilde
authors: M
authors: Balbi
authors: Valeria
authors: V
authors: Grazú
authors: Jesus M
authors: JM
authors: de La Fuente
authors: Gustavo
authors: G
authors: Egea
authors: Nikolaus
authors: N
authors: Plesnila
authors: Meritxell
authors: M
authors: Teixidó
authors: Ernest
authors: E
authors: Giralt
mesh_terms: D000818:Animals; D001692:Biological Transport; D001812:Blood-Brain Barrier / Q000378:metabolism*; D002417:Cattle; D002491:Central Nervous System Agents / Q000493:pharmacokinetics; D018920:Coculture Techniques; D042783:Endothelial Cells / Q000378:metabolism; D051379:Mice; D010447:Peptide Hydrolases / Q000737:chemistry; D010455:Peptides / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D010539:Permeability; D051381:Rats; D011990:Receptors, Transferrin / Q000187:drug effects; D013237:Stereoisomerism
chemical_list: D002491:Central Nervous System Agents; D010455:Peptides; D011990:Receptors, Transferrin; D010447:Peptide Hydrolases
keywords: blood-brain barrier; enantioselectivity; membranes; peptides; receptors