| 초록 |
The apoptosis inducing KLA peptide possesses an ability to disrupt mitochondrial membranes. However, KLA peptide lacks the ability to translocate efficiently into cells. Therefore, it requires the assistance of cell permeable materials for effective translocation into cells such as cell penetrating peptide (CPP). In an effort to improve the cell permeability of KLA, we introduced two Cys residues followed by oxidative S-S bond formation. One of dimers was efficiently internalized into cells at low concentration. Following translocation into cells, dimer is reductively converted into monomer, which then promotes disruption of the mitochondrial membrane. The results demonstrate that the strategy involving formation of bundle dimeric peptides is viable for the design of apoptosis inducing KLA peptide that translocate into cells at low concentrations. |
