Synthesis of Short Peptides with Perfluoroalkyl Side Chains and Evaluation of Their Cellular Uptake Efficiency

We have synthesized perfluoroalkyl-containing amino acids (RF-AA) and demonstrated that tripeptides composed of the RF-AA have high cellular uptake efficiency. Furthermore, the absolute configuration of RF-AA affected the uptake efficiency due to the change in its ability to form nanoparticles. We anticipate that these findings provide the foundation for the development of efficient cell-penetrating peptide (CPP). The cover picture shows tripeptides with perfluoroalkyl groups labeled with hydrophilic dyes that form particles in water and are efficiently taken up into cells. More information can be found in the Research Article by K. Aikawa et al.