The Effects of Lipidation on a TAT-Containing Peptide-Based Inhibitor of PSD-95
Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
Stability and cell permeability are critical parameters in the development of peptide therapeutics. Conjugation to fatty acids and cell-penetrating peptides, such as TAT (YGRKKRRQRRR), are established strategies to increase peptide stability and permeation, respectively. Here, we prepared lipidated analogues of a potent TAT-containing dimeric peptidebased inhibitor of the intracellular scaffolding protein PSD-95, an emerging drug target in ischaemic stroke. Lipidation increased peptide stability in vitro and in vivo. Combining both lipidation and conjugation to TAT improved brain/plasma ratios, but caused acute toxic effects due to the potent haemolytic activity of the TAT-lipid moiety.
Originalsprog | Engelsk |
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Tidsskrift | Australian Journal of Chemistry |
Vol/bind | 73 |
Udgave nummer | 4 |
Sider (fra-til) | 307-311 |
Antal sider | 5 |
ISSN | 0004-9425 |
DOI | |
Status | Udgivet - 2020 |
ID: 247213063