Article
Novel Keap1-Nrf2 Protein-Protein Interaction Inhibitor UBE-1099 Ameliorates Progressive Phenotype in Alport Syndrome Mouse Model.
Kidney360 - 28 Apr 2022
Kaseda Shota, Sannomiya Yuya, Horizono Jun, Kuwazuru Jun, Suico Mary Ann, Ogi Sayaka, Sasaki Ryoko, Sunamoto Hidetoshi, Fukiya Hirohiko, Nishiyama Hayato, Kamura Misato, Niinou Saki, Koyama Yuimi, Nara Futoshi, Shuto Tsuyoshi, Onuma Kazuhiro, Kai Hirofumi
Abstract excerpt
Background: Bardoxolone methyl activates nuclear factor erythroid 2-related factor 2 (Nrf2) via covalent binding and irreversible inhibition of Kelch-like ECH-associated protein 1 (Keap1), the negative regulator of Nrf2. Ongoing clinical trials of bardoxolone methyl show promising effects for patients with CKD. However, the direct inhibition of Keap1-Nrf2 protein-protein interaction (PPI) as an approach to...
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