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(a) Synthesis of the lipidated pepstatin A (LPA): a PEGylated lipid was conjugated to the cathepsin D inhibitor pepstatin A through the reaction between a corresponding amine and carboxyl groups using standard coupling reagents. (b) A schematic representation of the pepstatin A liposomal system (PepA-L): lipidated pepstatin A was inserted into the lipid bilayer of liposomes, which also contained a fluorescent dye (rhodamine).
