Fig. 3. MDM2 binding peptides with photoswitchable constraints that exhibit distinct thermodynamic signatures; (a) structures of both “open” and “closed” DAE stapled photoisomers, (R = H or Me, n = 1 or 2) used by Spring and co-workers to target the p53/MDM2 interaction; (b) crystal structure of MDM2 (blue) in complex with the highest affinity “open” analogue (red, PDB: 6Y4Q). Residues known to be crucial for binding to MDM2 are shown as sticks: Phe3, Trp7, Leu10, with the linker shown in orange making direct or H2O-mediated contacts (dashed lines) with MDM2.52.
