title: Dual system for the central nervous system targeting and blood-brain barrier transport of a selective prolyl oligopeptidase inhibitor.
abstract: Less than 2% of all potential neurotherapeutics cross the blood-brain barrier (BBB). Here, we sought to build a construct with the capacity to cross this barrier, to behave as a chemical delivery system, and, once inside the central nervous system, to be transformed and then act as an enzyme inhibitor. With all this in mind, here, we describe the entire process to obtain such a compound, from the initial candidate selection to preparation of the compound library and posterior evaluation and final selection of the most promising candidates in terms of selectivity, serum stability, and BBB-transport.
authors.affiliation: Institute for Research in Biomedicine (IRB Barcelona), Barcelona Science Park, Baldiri Reixac 10, Barcelona, 08028, Spain.
authors.forename: Meritxell
authors.initials: M
authors.lastname: Teixidó
authors.forename: Esther
authors.initials: E
authors.lastname: Zurita
authors.forename: Laura
authors.initials: L
authors.lastname: Mendieta
authors.forename: Benjamí
authors.initials: B
authors.lastname: Oller-Salvia
authors.forename: Roger
authors.initials: R
authors.lastname: Prades
authors.forename: Teresa
authors.initials: T
authors.lastname: Tarragó
authors.forename: Ernest
authors.initials: E
authors.lastname: Giralt
mesh_terms: D001692:Biological Transport; D001812:Blood-Brain Barrier; D006801:Humans
keywords: blood-brain barrier; central nervous system; diketopiperazine; drug delivery; enzyme inhibitor