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Fig. 1 | Molecular Cancer

Fig. 1

From: Proteolysis-targeting chimeras (PROTACs) in cancer therapy

Fig. 1

The mechanism of PROTACs based on the UPS. UPS consists of specific enzymes (E1, E2 and E3) modifying proteins with ubiquitin and the proteasome degrading the ubiquitin-tagging proteins. PROTAC contains a POI ligand, an E3 ligand and a linker. The E3-PROTAC-POI ternary complex induces the polyubiquitination and proteasome-mediated degradation of POIs. The presented PROTAC is BRD4 degrader MZ1 that is composed of POI ligand JQ1 (red) and E3 ligand VHL-1 (yellow)

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