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靶向炎症反应:选择性糖皮质激素受体调节剂的应用。

Targeting inflammation using selective glucocorticoid receptor modulators.

机构信息

Laboratory for Eukaryotic Gene Expression & Signal Transduction (LEGEST), Department of Physiology, Ghent University, K.L. Ledeganckstraat 35, B-9000 Ghent, Belgium.

出版信息

Curr Opin Pharmacol. 2010 Aug;10(4):497-504. doi: 10.1016/j.coph.2010.04.007. Epub 2010 May 20.

Abstract

Glucocorticoids have been used since several decades in a variety of diseases in view of their potent anti-inflammatory properties. Nevertheless, the widespread use of glucocorticoids is hampered by the risk of side effects. Because the effects of glucocorticoids are mediated at large through interaction with the glucocorticoid receptor, which results in anti-inflammatory effects as well as side effects, much attention has been given to understanding the molecular regulation. Over the past decade, remarkable progress has been made in the mechanisms mediating glucocorticoid receptor dependent gene regulation. In this review we provide an overview of recent progress in understanding the mode of action of glucocorticoids and novel strategies to dissociate anti-inflammatory from metabolic side effects.

摘要

几十年来,由于糖皮质激素具有强大的抗炎特性,已在多种疾病中得到应用。然而,由于存在副作用的风险,糖皮质激素的广泛应用受到了阻碍。由于糖皮质激素的作用主要通过与糖皮质激素受体相互作用介导,从而产生抗炎作用和副作用,因此人们非常关注对其分子调控的理解。在过去的十年中,介导糖皮质激素受体依赖性基因调控的机制方面取得了显著进展。在这篇综述中,我们概述了理解糖皮质激素作用模式和分离抗炎与代谢副作用的新策略方面的最新进展。

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