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@article{Beard:2019:10.1039/C9SC04024B,
author = {Beard, R and Gaboriau, D and Gee, A and Tate, E},
doi = {10.1039/C9SC04024B},
journal = {Chemical Science},
pages = {10772--10778},
title = {Chemical biology tools for probing transcytosis at the blood-brain barrier},
url = {http://dx.doi.org/10.1039/C9SC04024B},
volume = {10},
year = {2019}
}
TY - JOUR
AB - Absorptive- and receptor-mediated transcytosis (AMT/RMT) are widely studied strategies to deliver therapeutics across the blood–brain barrier (BBB). However, an improved understanding of the mechanism surrounding trafficking is required that could promote delivery. Accordingly, we designed a flexible platform that merged AMT and RMT motifs on a single scaffold to probe various parameters (ligand, affinity, valency, position) in a screening campaign. During this process we adapted an in vitro BBB model to reliably rank transcytosis of the vehicle library. Our results demonstrate heightened uptake and trafficking for the shuttles, with a structure–activity relationship for transcytosis emerging. Notably, due to their small size, the majority of shuttles demonstrated increased permeation compared to transferrin, with the highest performing shuttle affording a 4.9-fold increase. Consequently, we have identified novel peptide conjugates that have the capacity to act as promising brain shuttles.
AU - Beard,R
AU - Gaboriau,D
AU - Gee,A
AU - Tate,E
DO - 10.1039/C9SC04024B
EP - 10778
PY - 2019///
SN - 2041-6520
SP - 10772
TI - Chemical biology tools for probing transcytosis at the blood-brain barrier
T2 - Chemical Science
UR - http://dx.doi.org/10.1039/C9SC04024B
UR - http://hdl.handle.net/10044/1/74477
VL - 10
ER -