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白三烯合成抑制剂与拮抗剂:利弊分析

Leukotriene synthesis inhibitors versus antagonists: the pros and cons.

作者信息

Steinke John W, Culp Jeffrey A

机构信息

Asthma and Allergic Disease Center, Beirne Carter Center for Immunology Research, University of Virginia Health System, Charlottesville, VA 22908-1355, USA.

出版信息

Curr Allergy Asthma Rep. 2007 May;7(2):126-33. doi: 10.1007/s11882-007-0010-6.

DOI:10.1007/s11882-007-0010-6
PMID:17437683
Abstract

It has been recognized for many years that leukotrienes play an important role in mediating various effects of the allergic reaction. Recent evidence has shown that they play a role in other diseases. Leukotrienes can be separated into the fairly well-characterized cysteinyl leukotrienes and the less well-characterized leukotriene B(4). Effects of the leukotrienes are mediated through receptors that are expressed on a variety of cell types and can be modulated based on the inflammatory environment present. The pharmaceutical industry has long been interested in blocking leukotriene action. As such, two approaches have been developed that led to drugs approved for treating allergic disease. The most widely used class is the cysteinyl type 1 receptor antagonists, which block binding of the cysteinyl leukotrienes to the cell. The second class is an inhibitor of the 5-lipoxygenase enzyme that prevents synthesis of both the cysteinyl leukotrienes and leukotriene B(4). This review focuses on the role that leukotrienes play in various diseases, with the emphasis on allergic diseases, and considers the rationale for choosing either a leukotriene antagonist or synthesis inhibitor as a treatment option.

摘要

多年来人们已经认识到白三烯在介导过敏反应的各种效应中起重要作用。最近的证据表明它们在其他疾病中也发挥作用。白三烯可分为特征较为明确的半胱氨酰白三烯和特征不太明确的白三烯B4。白三烯的效应是通过在多种细胞类型上表达的受体介导的,并且可根据存在的炎症环境进行调节。制药行业长期以来一直对阻断白三烯作用感兴趣。因此,已经开发出两种方法,从而产生了被批准用于治疗过敏性疾病的药物。使用最广泛的一类是半胱氨酰1型受体拮抗剂,它可阻断半胱氨酰白三烯与细胞的结合。第二类是5-脂氧合酶抑制剂,它可阻止半胱氨酰白三烯和白三烯B4的合成。本综述重点关注白三烯在各种疾病中的作用,尤其是过敏性疾病,并考虑选择白三烯拮抗剂或合成抑制剂作为治疗选择的基本原理。

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