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阿司匹林及其主要代谢产物水杨酸的新发现靶点。

Newly Identified Targets of Aspirin and Its Primary Metabolite, Salicylic Acid.

作者信息

Klessig Daniel F

机构信息

Boyce Thompson Institute, Cornell University , Ithaca, New York.

出版信息

DNA Cell Biol. 2016 Apr;35(4):163-6. doi: 10.1089/dna.2016.3260. Epub 2016 Mar 8.

Abstract

Salicylic acid (SA) is a plant hormone, which influences several physiological processes, and is a critical modulator of multiple levels of immunity in plants. Several high-throughput screens, which were developed to identify SA-binding proteins through which SA mediates its many physiological effects in plants, uncovered several novel targets of aspirin and its primary metabolite, SA, in humans. These include glyceraldehyde 3-phosphate dehydrogenase (GAPDH) and high mobility group box 1 (HMGB1), two proteins associated with some of the most prevalent and devastating human diseases. In addition, natural and synthetic SA derivatives were discovered, which are much more potent than SA at inhibiting the disease-associated activities of these targets.

摘要

水杨酸(SA)是一种植物激素,它影响多种生理过程,并且是植物多层次免疫的关键调节因子。为了鉴定水杨酸结合蛋白(SA通过这些蛋白介导其在植物中的多种生理效应)而开展的多项高通量筛选,揭示了阿司匹林及其主要代谢产物水杨酸在人体内的几个新靶点。其中包括甘油醛-3-磷酸脱氢酶(GAPDH)和高迁移率族蛋白B1(HMGB1),这两种蛋白质与一些最常见且具有破坏性的人类疾病有关。此外,还发现了天然和合成的水杨酸衍生物,它们在抑制这些靶点与疾病相关的活性方面比水杨酸更有效。

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