The Effects of Lipidation on a TAT-Containing Peptide-Based Inhibitor of PSD-95
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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.
Original language | English |
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Journal | Australian Journal of Chemistry |
Volume | 73 |
Issue number | 4 |
Pages (from-to) | 307-311 |
Number of pages | 5 |
ISSN | 0004-9425 |
DOIs | |
Publication status | Published - 2020 |
- CELL-PENETRATING PEPTIDES, GLUCAGON-LIKE PEPTIDE-1, IN-VITRO, PROTRACTION, DERIVATIVES, DESIGN, ANTIBACTERIAL, MECHANISM, EFFICACY, INSULIN
Research areas
ID: 247213063