Ontology highlight
ABSTRACT:
SUBMITTER: Fadzen CM
PROVIDER: S-EPMC5818988 | biostudies-literature | 2017 Nov
REPOSITORIES: biostudies-literature
Journal of the American Chemical Society 20171030 44
Here we describe the utility of peptide macrocyclization through perfluoroaryl-cysteine S<sub>N</sub>Ar chemistry to improve the ability of peptides to cross the blood-brain barrier. Multiple macrocyclic analogues of the peptide transportan-10 were investigated that displayed increased uptake in two different cell lines and improved proteolytic stability. One of these analogues (M13) exhibited substantially increased delivery across a cellular spheroid model of the blood-brain barrier. Through e ...[more]