Click RWmix – Click Peptides

Cell penetrating peptides (CPP) are a keen area of molecule design to create the ideal vector for transporting macromolecule cargo into the cell. There is also a crossover of CPP acting as antimicrobial peptides (AMP) due to their ability to permeabilise the lipid membrane. AMPs are now being considered as a tool against the rise of antibiotic-resistant bacteria. CPPs and AMPS tend to be 10 – 30 amino acids long, cationic, and rich in arginine and tryptophan. The RWR motif has been used to generate de novo CPP/AMP peptides with improved functions. Of these, RWmix was shown to have the highest cellular uptake against other RWR synthetics, the lowest cytotoxicity and significant antimicrobial activity. RWmix 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-RWmix allows a wide variety of applications particularly for conjugation, modification, and peptide design.