Abstract

Peptides and phospholipids are important macromolecules in both the chemistry and biology fields, but phospholipopeptides are barely found in nature and have not been studied. Here, we report a novel and efficient approach to the synthesis of phospholipidpeptides. By utilizing cross‐linkers, phospholipopeptides from peptides with varied sequences and lengths were produced from phosphatidylethanolamine at high (>90%) yield, mild conditions and good applied scopes for multiple substrates. Synthetic phospholipopeptides containing bioactive peptide sequences may serve as therapeutics for a wide range of biomedical applications.Practical applications: Phospholipopeptides are prone to hydrolysis by the endogenous phospholipase activity in cells. Synthetic phospholipopeptides containing a bioactive peptide sequences may serve as therapeutics for a wide range of biomedical applications.Cysteine‐containing peptides of varied sequences and lengths were linked to the heads of phosphatidylethanolamine through the amino group to form phospholipopeptides.

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