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选择性糖皮质激素受体调节剂(SGRMs)发现方面的最新进展。

Recent developments in the discovery of selective glucocorticoid receptor modulators (SGRMs).

作者信息

Hudson Andrew R, Roach Steven L, Higuchi Robert I

机构信息

Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA.

出版信息

Curr Top Med Chem. 2008;8(9):750-65. doi: 10.2174/156802608784535048.

DOI:10.2174/156802608784535048
PMID:18537686
Abstract

Steroidal glucocorticoids are widely prescribed for the treatment of a variety of inflammatory and autoimmune diseases. Although they are effective, the side-effects associated with chronic glucocorticoid treatment, such as osteoporosis and hyperglycemia, can severely limit their long-term use. Hence, there is a need to develop new effective anti-inflammatory agents for systemic use which are dissociated from their unwanted side effects.

摘要

甾体糖皮质激素被广泛用于治疗多种炎症和自身免疫性疾病。尽管它们有效,但与长期糖皮质激素治疗相关的副作用,如骨质疏松和高血糖,会严重限制其长期使用。因此,需要开发新的全身性有效抗炎药物,使其与不良副作用脱钩。

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Recent developments in the discovery of selective glucocorticoid receptor modulators (SGRMs).选择性糖皮质激素受体调节剂(SGRMs)发现方面的最新进展。
Curr Top Med Chem. 2008;8(9):750-65. doi: 10.2174/156802608784535048.
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Recent progress in the discovery of novel glucocorticoid receptor modulators.新型糖皮质激素受体调节剂发现方面的最新进展。
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Glucocorticoid action and the development of selective glucocorticoid receptor ligands.糖皮质激素作用与选择性糖皮质激素受体配体的研发
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Dissociated glucocorticoid receptor ligands.解离型糖皮质激素受体配体
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Efficacy and safety of selective glucocorticoid receptor modulators in comparison to glucocorticoids in arthritis, a systematic review.与糖皮质激素相比,选择性糖皮质激素受体调节剂在关节炎中的疗效和安全性:一项系统评价
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Discovery and optimization of novel, non-steroidal glucocorticoid receptor modulators.新型非甾体糖皮质激素受体调节剂的发现与优化
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Drug insight: selective agonists and antagonists of the glucocorticoid receptor.药物洞察:糖皮质激素受体的选择性激动剂和拮抗剂
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JTP-117968, a novel selective glucocorticoid receptor modulator, exhibits improved transrepression/transactivation dissociation.JTP-117968是一种新型选择性糖皮质激素受体调节剂,具有改善的反式抑制/反式激活解离特性。
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Natural and synthetic compounds as dissociated agonists of glucocorticoid receptor.天然和合成化合物作为糖皮质激素受体的分离激动剂。
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Improved Glucocorticoid Receptor Ligands: Fantastic Beasts, but How to Find Them?改善的糖皮质激素受体配体:神奇动物,又该如何寻找?
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引用本文的文献

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Yin Yang 1 promotes hepatic gluconeogenesis through upregulation of glucocorticoid receptor.阴阳 1 通过上调糖皮质激素受体促进肝糖异生。
Diabetes. 2013 Apr;62(4):1064-73. doi: 10.2337/db12-0744. Epub 2012 Nov 27.
2
Anti-inflammatory effects of selective glucocorticoid receptor modulators are partially dependent on up-regulation of dual specificity phosphatase 1.选择性糖皮质激素受体调节剂的抗炎作用部分依赖于双特异性磷酸酶 1 的上调。
Br J Pharmacol. 2012 Feb;165(4b):1124-36. doi: 10.1111/j.1476-5381.2011.01574.x.
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Iatrogenic Cushing syndrome caused by ocular glucocorticoids in a child.
儿童眼部糖皮质激素所致医源性库欣综合征
BMJ Case Rep. 2009;2009. doi: 10.1136/bcr.11.2008.1224. Epub 2009 May 8.
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Crosstalk in inflammation: the interplay of glucocorticoid receptor-based mechanisms and kinases and phosphatases.炎症中的串扰:基于糖皮质激素受体的机制与激酶和磷酸酶的相互作用。
Endocr Rev. 2009 Dec;30(7):830-82. doi: 10.1210/er.2009-0013. Epub 2009 Nov 4.
5
Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor.利用受体上一个新的结合位点的高效非甾体糖皮质激素激动剂的设计与X射线晶体结构
Proc Natl Acad Sci U S A. 2009 Oct 27;106(43):18114-9. doi: 10.1073/pnas.0909125106. Epub 2009 Oct 12.