Revvity HTRF Human KEAP1 Binding Kit, 100,000 Assay Points

The KEAP1-NRF2-ARE pathway plays an important role in the response to oxidative stress and in maintaining redox homeostasis. KEAP1 (Kelch-like ECH-associated protein 1) is an adaptor subunit of the Cullin 3-based E3 ubiquitin ligase, involved in oxidative stress response. By promoting UPS mediated degradation, KEAP1 controls the expression level of NRF2, a key transcription that regulates the expression of antioxidant proteins, therefore ensuring cells protection from oxidative stress. Sustained activation of NRF2 has been associated with cancer resistance, and its inhibition has been shown to weaken drug 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 the removal of undesired proteins (e.g. NRF2) involved in various diseases such as cancers, neurodegenerative diseases, and metabolic disorders.