Figure 1.

Schematic diagram showing the mechanism of action of PROTAC technology (for this example, we used VHL E3 ubiquitin ligase to decompose the AR).

The PROTAC molecule is like a dumbbell, with a linker in the middle, a targeted protein ligand at one end, and an E3 ligase recognition moiety at the other end. The E3 ligase is recruited to the target protein (AR) by the PROTAC molecule, and then the ubiquitin-tagged target protein (AR) is recognized and degraded by the proteasome. The ubiquitin and PROTAC are subsequently recycled. AR: Androgen receptor; PROTAC: proteolysis-targeting chimeric molecule; VHL: von Hippel–Lindau.