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Kelch-like ECH-associated protein 1 (KEAP1) is an adaptor subunit of Cullin 3-based E3 ubiquitin ligase involved in oxidative stress response. By promoting UPS mediated degradation, KEAP1 controls the expression level of key proteins such as NRF2, a transcription factor controlling the expression of antioxidant proteins. Sustained activation of NRF2 has been associated to cancers resistance, and its inhibition has been shown to dampen drugs resistance. Targeted protein degradation (TPD) uses small molecules to recruit E3 ubiquitin ligases into the proximity of the targeted protein of interest, promoting its ubiquitination-dependent degradation. Exploiting KEAP1 inhibitors for the development of bifunctional Proteolysis-targeting chimeras (PROTACs) is expected to expand the toolbox of E3 ligases to removing undesired proteins (e.g., NRF2) involved in various diseases such as cancers, neurodegenerative diseases, and metabolic disorders.
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