Please read Dr. Aleksunes’ article in Bioorganic and Medicinal Chemistry titled, “Optimization of 1,4-bis(arylsulfonamido)naphthalene-N,N’-diacetic acids as inhibitors of Keap1-Nrf2 protein-protein interaction to suppress neuroinflammation.“
Continuous oxidative stress conditions have been implicated in the pathogenesis of chronic inflammation, even leading to the progression of a wide range of diseases, such as neurodegenerative disorders, chronic obstructive pulmonary disorder (COPD), chronic kidney disease, and cancer. In particular, neurodegeneration has been considered to be irreversible; available treatments only alleviate symptoms and are less effective in advanced diseases. Given the fact that nuclear factor erythroid 2-related factor 2 (Nrf2) is a master regulator of the antioxidant cellular defense system, Nrf2 could exert a protective effect against neurodegeneration exacerbated by oxidative stress. Indeed, it was demonstrated that Nrf2 plays a significant role in modulating microglial dynamics in a chronic model of Parkinson’s disease (PD). To read the full article.
Optimization of 1,4-bis(arylsulfonamido)naphthalene-N,N’-diacetic acids as inhibitors of Keap1-Nrf2 protein-protein interaction to suppress neuroinflammation. Abed DA, Lee S, Wen X, Ali AR, Mangipudy V, Aleksunes LM, Hu L. Bioorg Med Chem. 2021 Aug 15;44:116300. PMID: 34252790 PMCID: PMC8349900 DOI: 1016/j.bmc.2021.116300 Epub 2021 Jul 1.