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Non-covalent direct inhibition of the Keap1-Nrf2 PPI resulting in upregulation of ARE-gene expression. Thus, increase ARE-controlled cytoprotective oxidative stress response enzymes in the development of therapeutic and preventive agents for a number of diseases and conditions.
Invention Summary:
The Keap1-Nrf2-ARE system could protect cells against oxidative stress involving in many diseases. Targeting Keap1-Nrf2 protein-proteins interaction (PPI) is a promising therapeutic strategy for oxidative stress-related diseases. Many of the known Keap1-Nrf2 PPI inhibitors are considered electrophilic indirect inhibitors and are not selective, which may cause off-target toxicity.
Rutgers researchers have found diverse classes of potent small molecule inhibitors with unique scaffolds and direct targets. With four novel scaffolds, these new compounds are reversible, specific, and have higher potency for Keap1-Nrf2 PPI inhibition. Providing more specific targets and causing fewer side effects. Our invention gives the potential therapeutic options for many oxidative stress-related diseases, including colitis, chronic kidney disease, pulmonary fibrosis, chronic obstructive pulmonary disorder (COPD), Alzheimer’s and Parkinson’s Disease, and the prevention of cancer.
Market Applications:
Selective therapeutic for:
Advantages:
Publications:
Intellectual Property & Development Status: Provisional application filed. Patent pending. Available for licensing and/or research collaboration. For any business development and other collaborative partnerships, contact: marketingbd@research.rutgers.edu
