• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

糖原合酶激酶-3(GSK-3)抑制剂已进入临床应用。

Glycogen synthase kinase-3 (GSK-3) inhibitors reach the clinic.

作者信息

Medina Miguel, Castro Ana

机构信息

Neuropharma SA, Avenida de la Industria 52, 28760 Tres Cantos, Madrid, Spain.

出版信息

Curr Opin Drug Discov Devel. 2008 Jul;11(4):533-43.

PMID:18600569
Abstract

It is just over a quarter of a century since the original identification and characterization of glycogen synthase kinase-3 (GSK-3), a major protein kinase that is involved in the regulation of glucose metabolism. GSK-3 modulates the function of a diverse series of proteins, as well as being associated with a wide variety of human disorders, including neurodegenerative diseases, stroke, bipolar disorder, diabetes and cancer. Not surprisingly, GSK-3 has attracted significant attention as a therapeutic target and as a means to understand the molecular basis of these disorders. Small-molecule GSK-3 inhibitors have now started to reach clinical development for the treatment of various disorders.

摘要

糖原合酶激酶-3(GSK-3)最初被鉴定和表征距今不过二十五年多一点,它是一种主要的蛋白激酶,参与葡萄糖代谢的调节。GSK-3调节一系列不同蛋白质的功能,还与多种人类疾病相关,包括神经退行性疾病、中风、双相情感障碍、糖尿病和癌症。不出所料,GSK-3作为治疗靶点以及理解这些疾病分子基础的一种手段,已引起了极大关注。小分子GSK-3抑制剂现已开始进入治疗各种疾病的临床开发阶段。

相似文献

1
Glycogen synthase kinase-3 (GSK-3) inhibitors reach the clinic.糖原合酶激酶-3(GSK-3)抑制剂已进入临床应用。
Curr Opin Drug Discov Devel. 2008 Jul;11(4):533-43.
2
Preclinical efficacy on GSK-3 inhibitors: towards a future generation of powerful drugs.GSK-3抑制剂的临床前疗效:迈向新一代强效药物
Med Res Rev. 2008 Sep;28(5):773-96. doi: 10.1002/med.20119.
3
Glycogen synthase kinase 3 (GSK-3) inhibitors as new promising drugs for diabetes, neurodegeneration, cancer, and inflammation.糖原合酶激酶3(GSK-3)抑制剂作为治疗糖尿病、神经退行性疾病、癌症和炎症的新型有前景药物。
Med Res Rev. 2002 Jul;22(4):373-84. doi: 10.1002/med.10011.
4
[A new target for diabetes therapy: advances in the research of glycogen synthase kinase-3 inhibitors].糖尿病治疗的新靶点:糖原合酶激酶-3抑制剂的研究进展
Yao Xue Xue Bao. 2007 Dec;42(12):1227-31.
5
QSAR modeling of the inhibition of glycogen synthase kinase-3.糖原合酶激酶-3抑制作用的定量构效关系建模
Bioorg Med Chem. 2006 Jul 15;14(14):4987-5002. doi: 10.1016/j.bmc.2006.03.009. Epub 2006 May 2.
6
Design and synthesis of 7-hydroxy-1H-benzoimidazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.7-羟基-1H-苯并咪唑衍生物作为糖原合酶激酶-3β新型抑制剂的设计与合成
Bioorg Med Chem Lett. 2007 Oct 15;17(20):5686-9. doi: 10.1016/j.bmcl.2007.07.056. Epub 2007 Aug 19.
7
3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.3-(7-氮杂吲哚基)-4-芳基马来酰亚胺作为糖原合酶激酶-3的强效、选择性抑制剂。
Bioorg Med Chem Lett. 2004 Jun 21;14(12):3245-50. doi: 10.1016/j.bmcl.2004.03.090.
8
Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3α.鉴定糖原合酶激酶-3 的抑制剂,具有选择性针对糖原合酶激酶-3α 的作用。
J Med Chem. 2012 May 10;55(9):4407-24. doi: 10.1021/jm300309a. Epub 2012 May 1.
9
CDK/GSK-3 inhibitors as a new approach for the treatment of proliferative renal diseases.CDK/GSK-3抑制剂作为治疗增殖性肾脏疾病的新方法。
Drug News Perspect. 2006 Jul-Aug;19(6):325-8. doi: 10.1358/dnp.2006.19.6.985939.
10
Organometallic compounds with biological activity: a very selective and highly potent cellular inhibitor for glycogen synthase kinase 3.具有生物活性的有机金属化合物:一种对糖原合酶激酶3具有高度选择性和强效的细胞抑制剂。
Chembiochem. 2006 Sep;7(9):1443-50. doi: 10.1002/cbic.200600117.

引用本文的文献

1
Alzheimer's Disease: An Overview of Major Hypotheses and Therapeutic Options in Nanotechnology.阿尔茨海默病:纳米技术中的主要假说与治疗选择概述
Nanomaterials (Basel). 2020 Dec 29;11(1):59. doi: 10.3390/nano11010059.
2
Tau phosphorylation by glycogen synthase kinase 3β modulates enzyme acetylcholinesterase expression.糖原合酶激酶 3β 通过磷酸化 Tau 调节酶乙酰胆碱酯酶的表达。
J Neurochem. 2021 Jun;157(6):2091-2105. doi: 10.1111/jnc.15189. Epub 2020 Oct 4.
3
The selective GSK3 inhibitor, SAR502250, displays neuroprotective activity and attenuates behavioral impairments in models of neuropsychiatric symptoms of Alzheimer's disease in rodents.
选择性 GSK3 抑制剂 SAR502250 具有神经保护活性,并可减轻阿尔茨海默病神经精神症状模型中啮齿动物的行为损伤。
Sci Rep. 2019 Dec 2;9(1):18045. doi: 10.1038/s41598-019-54557-5.
4
Aberrant expression of glycogen synthase kinase-3β in human breast and head and neck cancer.糖原合成酶激酶-3β在人类乳腺癌及头颈癌中的异常表达。
Oncol Lett. 2018 Nov;16(5):6437-6444. doi: 10.3892/ol.2018.9483. Epub 2018 Sep 21.
5
Lithium Inhibits GSK3β and Augments GluN2A Receptor Expression in the Prefrontal Cortex.锂抑制前额叶皮质中的糖原合成酶激酶3β并增强谷氨酸N2A受体表达。
Front Cell Neurosci. 2018 Feb 1;12:16. doi: 10.3389/fncel.2018.00016. eCollection 2018.
6
Radiosynthesis and in Vivo Evaluation of [C]A1070722, a High Affinity GSK-3 PET Tracer in Primate Brain.[C]A1070722 是一种高亲和力 GSK-3 PET 示踪剂,在灵长类动物大脑中的放射合成与体内评估。
ACS Chem Neurosci. 2017 Aug 16;8(8):1697-1703. doi: 10.1021/acschemneuro.6b00376. Epub 2017 May 17.
7
Molecular Pathways: Revisiting Glycogen Synthase Kinase-3β as a Target for the Treatment of Cancer.分子途径:重新审视糖原合酶激酶-3β作为癌症治疗靶点
Clin Cancer Res. 2017 Apr 15;23(8):1891-1897. doi: 10.1158/1078-0432.CCR-15-2240. Epub 2017 Jan 4.
8
Structural basis of GSK-3 inhibition by N-terminal phosphorylation and by the Wnt receptor LRP6.N端磷酸化及Wnt受体LRP6对糖原合酶激酶3(GSK-3)抑制作用的结构基础
Elife. 2014 Mar 18;3:e01998. doi: 10.7554/eLife.01998.
9
Neurotrophic natural products: chemistry and biology.神经营养天然产物:化学与生物学
Angew Chem Int Ed Engl. 2014 Jan 20;53(4):956-87. doi: 10.1002/anie.201302268. Epub 2013 Dec 18.
10
Neuronal apoptosis and motor deficits in mice with genetic inhibition of GSK-3 are Fas-dependent.基因抑制 GSK-3 的小鼠中神经元凋亡和运动缺陷依赖于 Fas。
PLoS One. 2013 Aug 5;8(8):e70952. doi: 10.1371/journal.pone.0070952. Print 2013.