Rational Tuning of Intracellular Release Kinetics in PROTAC–Peptide Conjugates via Positional Modulation of Functional Peptide Domains
Proteolysis-targeting chimeras (PROTACs) can induce degradation of otherwise challenging proteins, but their large size and unfavorable physicochemical properties often limit cellular delivery. We designed PROTAC–peptide conjugates containing a nona-arginine cell-penetrating peptide (R9), a redox-sensitive disulfide...