A linker approach to phospholipopeptides

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.