Click MAP – Click Peptides

Cell penetrating peptides (CPP) are a useful tool for drug delivery, but their cell-specific uptake is still being improved. Work with the model amphipathic peptide (MAP) has been important in this field. CPP MAP is an amphipathic α-helix and has been well characterised for its ability to spontaneously permeate the cell membrane by interacting with the lipid bilayer. As a CPP, MAP causes increased membrane permeability and a degree of cell leakage. MAP is being extensively studied to optimise drug delivery in numerous cell lines with the target of creating a viable clinical method. Interestingly, the CPP function of MAP also provides it with bactericidal properties by effecting the membrane permeability. MAP is a potent antimicrobial peptide (AMP) against gram negative Neisseria meningitidis, the pathogen of meningococcal disease. MAP is provided here with a N-terminal alkyne attachment. Two of the most regularly encountered functional groups for click chemistry are azides and alkynes, and the azide-alkyne cycloaddition has become the most popular click reaction. The use of click chemistry with alkyne-MAP allows a wide variety of applications particularly for conjugation, modification, and peptide design.