Department of Experimental Medicine, University of Campania "Luigi Vanvitelli", Via Costantinopoli, 16, 80138 Naples, Italy.
Department of Pharmacy, University of Naples Federico II, Naples, Italy.
Eur J Med Chem. 2018 Jun 10;153:65-72. doi: 10.1016/j.ejmech.2017.10.020. Epub 2017 Oct 10.
The products of 5-lipoxygenase are synthesized and released in the airway when an asthmatic reaction occurs. 5-lipoxygenase via arachidonic acid metabolism produces leukotrienes that mediate bronchoconstriction and inflammatory modifications essential in the pathophysiology of asthma. Until to now, only one approved 5-LO inhibitor, zileuton, can be found as a potential therapy for asthma. With the increasing number of indications for anti-leukotriene (anti-LT) drugs, the development of 5-LO inhibitor agents becomes increasingly important. The present MiniReview reports an update on 5-LO inhibitors currently under clinical investigation. In addition, the latest advances focused on the development of new 5-lipoxygenase inhibitors as asthma anti-inflammatory agents are also discussed.
当哮喘反应发生时,5-脂氧合酶的产物在气道中被合成并释放。5-脂氧合酶通过花生四烯酸代谢产生白三烯,介导支气管收缩和炎症改变,这些改变在哮喘的病理生理学中是必不可少的。到目前为止,只有一种批准的 5-LO 抑制剂齐留通(zileuton)被发现可作为哮喘的潜在治疗药物。随着抗白三烯(anti-LT)药物适应证的不断增加,5-LO 抑制剂的开发变得越来越重要。本综述报告了目前正在临床研究中的 5-LO 抑制剂的最新进展。此外,还讨论了作为哮喘抗炎药物的新型 5-脂氧合酶抑制剂的最新进展。