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• W2989136458 abstract "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 peptide-based 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." @default.
• W2989136458 created "2019-11-22" @default.
• W2989136458 creator A5060992391 @default.
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• W2989136458 date "2020-01-01" @default.
• W2989136458 modified "2023-09-27" @default.
• W2989136458 title "The Effects of Lipidation on a TAT-Containing Peptide-Based Inhibitor of PSD-95" @default.
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• W2989136458 doi "https://doi.org/10.1071/ch19392" @default.
• W2989136458 hasPublicationYear "2020" @default.
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