Author:
Xiao Qing-Ao,He Qian,Li Lun,Song Yinhong,Chen Yue-ran,Zeng Jun,Xia Xuan
Abstract
IKKε (inhibitor of nuclear factor kappa-B kinase ε) is a member of the noncanonical NF-κB pathway. It participates in the inflammatory response and innate immunity against bacteria. In recent decades, IKKε has been closely associated with metabolic regulation. Inhibition of the IKKε pathway can improve fat deposition in the liver, reduce subcutaneous fat inflammation, and improve liver gluconeogenesis in obesity. IKKε is expected to be a new therapeutic target for metabolic diseases such as nonalcoholic fatty liver disease, diabetes, and obesity. Herein, we summarize the structural characterization, physiological function, and pathological role of IKKε in metabolic diseases and small molecule inhibitors of IKKε.
Funder
National Natural Science Foundation of China
Natural Science Foundation of Hubei Province
Subject
Pharmacology (medical),Pharmacology
Reference94 articles.
1. Expanding the View of IKK: New Substrates and New Biology;Antonia;Trends Cel Biol,2021
2. NF-κB, Inflammation, and Metabolic Disease;Baker;Cell Metab,2011
3. 5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as Potent, Selective, Inhibitors of IKK-Epsilon Kinase;Bamborough;Bioorg. Med. Chem. Lett.,2006
4. Carboxylic Acid Derivatives of Amlexanox Display Enhanced Potency toward TBK1 and IKKε and Reveal Mechanisms for Selective Inhibition;Beyett;Mol. Pharmacol.
5. Design, Synthesis, and Biological Activity of Substituted 2-Amino-5-Oxo-5h-Chromeno[2,3-B]pyridine-3-Carboxylic Acid Derivatives as Inhibitors of the Inflammatory Kinases TBK1 and IKKε for the Treatment of Obesity;Beyett;Bioorg. Med. Chem.
Cited by
2 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献