Miller D K, Gillard J W, Vickers P J, Sadowski S, Léveillé C, Mancini J A, Charleson P, Dixon R A, Ford-Hutchinson A W, Fortin R
Department of Biochemistry and Molecular Biology, Merck Institute for Therapeutic Research, Rahway, New Jersey 07065.
Nature. 1990 Jan 18;343(6255):278-81. doi: 10.1038/343278a0.
Several inflammatory diseases, including asthma, arthritis and psoriasis are associated with the production of leukotrienes by neutrophils, mast cells and macrophages. The initial enzymatic step in the formation of leukotrienes is the oxidation of arachidonic acid by 5-lipoxygenase (5-LO) to leukotriene A4. Osteosarcoma cells transfected with 5-LO express active enzyme in broken cell preparations, but no leukotriene metabolites are produced by these cells when stimulated with the calcium ionophore A23187, indicating that an additional component is necessary for cellular 5-LO activity. A new class of indole leukotriene inhibitor has been described that inhibits the formation of cellular leukotrienes but has no direct inhibitory effect on soluble 5-LO activity. We have now used these potent agents to identify and isolate a novel membrane protein of relative molecular mass 18,000 which is necessary for cellular leukotriene synthesis.
包括哮喘、关节炎和牛皮癣在内的几种炎症性疾病都与中性粒细胞、肥大细胞和巨噬细胞产生白三烯有关。白三烯形成的初始酶促步骤是5-脂氧合酶(5-LO)将花生四烯酸氧化为白三烯A4。用5-LO转染的骨肉瘤细胞在破碎的细胞制剂中表达活性酶,但在用钙离子载体A23187刺激时,这些细胞不会产生白三烯代谢物,这表明细胞5-LO活性还需要一种额外的成分。已描述了一类新型的吲哚白三烯抑制剂,它能抑制细胞白三烯的形成,但对可溶性5-LO活性没有直接抑制作用。我们现在已使用这些强效试剂来鉴定和分离一种相对分子质量为18,000的新型膜蛋白,它是细胞白三烯合成所必需的。