201. Recent progress in Keap1-Nrf2 protein-protein interaction inhibitors
- Author
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Shuai Wen, Zhang Xin, Yu-Xiu Li, Zheng-Yu Jiang, Gao Xinxing, and Yi Mou
- Subjects
NF-E2-Related Factor 2 ,Regulator ,Peptide ,Computational biology ,medicine.disease_cause ,Therapeutic targeting ,digestive system ,environment and public health ,Protein–protein interaction ,Small Molecule Libraries ,Drug Discovery ,medicine ,Humans ,Pharmacology ,chemistry.chemical_classification ,Kelch-Like ECH-Associated Protein 1 ,Molecular Structure ,Chemistry ,Organic Chemistry ,General Medicine ,respiratory system ,KEAP1 ,Small molecule ,Keap1 nrf2 ,Peptides ,Oxidative stress ,Protein Binding ,Signal Transduction - Abstract
Therapeutic targeting the protein-protein interaction (PPI) of Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) and its main regulator, Kelch-like ECH-Associating protein 1 (Keap1) has been emerged as a feasible way to combat oxidative stress related diseases, due to the key role of Nrf2 in oxidative stress regulation. In recent years, many efforts have been made to develop potent Keap1-Nrf2 inhibitors with new chemical structures. Various molecules with diverse chemical structures have been reported and some compounds exhibit high potency. This review summarizes peptide and small molecule Keap1-Nrf2 inhibitors reported recently. We also highlight the pharmacological effects and discuss the possible therapeutic application of Keap1-Nrf2 inhibitors.
- Published
- 2020