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[前列腺素调节的当前主题 - 1. 诱导型环氧化酶COX - 2与选择性阻滞剂]

[Current topics in the regulation of prostanoids-1. Inducible cyclooxygenase COX-2 and selective blockers].

作者信息

Ohara M, Sawa T

机构信息

Department of Anesthesiology, Yokohama City University, School of Medicine.

出版信息

Masui. 1998 Nov;47(11):1325-32.

PMID:9852696
Abstract

Cyclooxygenases (COX) are prostaglandin synthases and are the main therapeutic targets for non-steroidal anti-inflammatory drugs. Recently it has been established that apart from the constitutive isoform, an inducible isoform of this enzyme is upregulated after injurious stimuli. The structures of the genes encoding these enzymes and protein structures have been determined, and with the utilization of knockout mice, the physiological properties of each isozyme are being revealed. COX-1 is responsible for the production of physiological levels of prostanoids, whereas COX-2 is upregulated during inflammatory states and produces prostanoids responsible for the generation of fever, pain or other inflammatory responses. Selective COX-2 blockers may be a safe and useful alternative in the treatment of inflammatory disorders, pain, and fever.

摘要

环氧化酶(COX)是前列腺素合成酶,是非甾体抗炎药的主要治疗靶点。最近已经确定,除了组成型同工型外,这种酶的诱导型同工型在损伤性刺激后会上调。编码这些酶的基因结构和蛋白质结构已经确定,并且通过利用基因敲除小鼠,每种同工酶的生理特性正在被揭示。COX-1负责生理性前列腺素水平的产生,而COX-2在炎症状态下上调,并产生导致发热、疼痛或其他炎症反应的前列腺素。选择性COX-2阻滞剂可能是治疗炎症性疾病、疼痛和发热的一种安全且有用的替代药物。

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