Department of Biochemistry, Graduate School of Medicine, Juntendo University, Tokyo, Japan.
Department of Life Science, Graduate School of Science, Okayama University of Science, Okayama, Japan.
J Clin Invest. 2018 Jul 2;128(7):2691-2701. doi: 10.1172/JCI97946. Epub 2018 May 14.
Leukotrienes, a class of arachidonic acid-derived bioactive molecules, are known as mediators of allergic and inflammatory reactions and considered to be important drug targets. Although an inhibitor of leukotriene biosynthesis and antagonists of the cysteinyl leukotriene receptor are clinically used for bronchial asthma and allergic rhinitis, these medications were developed before the molecular identification of leukotriene receptors. Numerous studies using cloned leukotriene receptors and genetically engineered mice have unveiled new pathophysiological roles for leukotrienes. This Review covers the recent findings on leukotriene receptors to revisit them as new drug targets.
白三烯是一类由花生四烯酸衍生的生物活性分子,已知其为过敏和炎症反应的介质,并被认为是重要的药物靶点。尽管白三烯生物合成抑制剂和半胱氨酰白三烯受体拮抗剂已用于治疗支气管哮喘和过敏性鼻炎,但这些药物是在白三烯受体的分子鉴定之前开发的。使用克隆的白三烯受体和基因工程小鼠进行的大量研究揭示了白三烯的新病理生理学作用。本综述涵盖了白三烯受体的最新研究发现,以重新将其视为新的药物靶点。