Figure 2.
The design of peptides in this study. R7 (hepta-arginine) is a cell-penetrating peptide. LCL (LCL-161) is a IAP ligand. To develop chimeric degraders, LCL-161 was conjugated to the ε-amino group of the N-terminal Lys residue of PERML and stPERML via an ethylene glycol-based linker, respectively. Combinations of (S)-pentenyl alanine (S5) are used for different positions of stapling the hydrocarbon linker, and employing S5, S5 at position i/i + 4 is the most common stapling position on the same face of helix turn.