• 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

The small molecule CLP257 does not modify activity of the K-Cl co-transporter KCC2 but does potentiate GABA receptor activity.

作者信息

Cardarelli Ross A, Jones Karen, Pisella Lucie I, Wobst Heike J, McWilliams Lisa J, Sharpe Paul M, Burnham Matthew P, Baker David J, Chudotvorova Ilona, Guyot Justine, Silayeva Liliya, Morrow Danielle H, Dekker Niek, Zicha Stephen, Davies Paul A, Holenz Jörg, Duggan Mark E, Dunlop John, Mather Robert J, Wang Qi, Medina Igor, Brandon Nicholas J, Deeb Tarek Z, Moss Stephen J

机构信息

AstraZeneca Tufts Laboratory for Basic and Translational Neuroscience, Boston, Massachusetts, USA.

Discovery Sciences, IMED Biotech Unit, AstraZeneca, Alderley Park, UK.

出版信息

Nat Med. 2017 Dec 7;23(12):1394-1396. doi: 10.1038/nm.4442.

DOI:10.1038/nm.4442
PMID:29216042
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7371006/
Abstract
摘要

相似文献

1
The small molecule CLP257 does not modify activity of the K-Cl co-transporter KCC2 but does potentiate GABA receptor activity.小分子CLP257不会改变钾氯协同转运体KCC2的活性，但会增强GABA受体的活性。
Nat Med. 2017 Dec 7;23(12):1394-1396. doi: 10.1038/nm.4442.
2
Reply to The small molecule CLP257 does not modify activity of the K-Cl co-transporter KCC2 but does potentiate GABA receptor activity.对小分子CLP257不改变钾氯共转运体KCC2的活性但能增强GABA受体活性的回应。
Nat Med. 2017 Dec 7;23(12):1396-1398. doi: 10.1038/nm.4449.
3
Brain-type creatine kinase activates neuron-specific K+-Cl- co-transporter KCC2.脑型肌酸激酶激活神经元特异性钾氯协同转运体KCC2。
J Neurochem. 2006 Jan;96(2):598-608. doi: 10.1111/j.1471-4159.2005.03560.x. Epub 2005 Nov 29.
4
Chloride homeostasis differentially affects GABA(A) receptor- and glycine receptor-mediated effects on spontaneous circuit activity in hippocampal cell culture.氯离子稳态对海马细胞培养中γ-氨基丁酸A（GABA(A)）受体和甘氨酸受体介导的自发回路活动的影响存在差异。
Neurosci Lett. 2006 Oct 2;406(1-2):11-6. doi: 10.1016/j.neulet.2006.06.064. Epub 2006 Aug 14.
5
Chloride extrusion enhancers as novel therapeutics for neurological diseases.氯离子外排增强剂：神经疾病治疗的新策略
Nat Med. 2013 Nov;19(11):1524-8. doi: 10.1038/nm.3356. Epub 2013 Oct 6.
6
GABA receptor dependent synaptic inhibition rapidly tunes KCC2 activity via the Cl-sensitive WNK1 kinase.GABA 受体依赖性突触抑制通过 Cl-敏感的 WNK1 激酶快速调节 KCC2 的活性。
Nat Commun. 2017 Nov 24;8(1):1776. doi: 10.1038/s41467-017-01749-0.
7
Could tuning of the inhibitory tone involve graded changes in neuronal chloride transport?抑制性调节是否涉及神经元氯离子转运的分级变化？
Neuropharmacology. 2015 Aug;95:321-31. doi: 10.1016/j.neuropharm.2015.03.026. Epub 2015 Apr 3.
8
Reduction of KCC2 expression and GABAA receptor-mediated excitation after in vivo axonal injury.体内轴突损伤后KCC2表达及GABAA受体介导的兴奋作用降低。
J Neurosci. 2002 Jun 1;22(11):4412-7. doi: 10.1523/JNEUROSCI.22-11-04412.2002.
9
Role of Cl- co-transporters in the excitation produced by GABAA receptors in juvenile bovine adrenal chromaffin cells.氯离子共转运体在幼年牛肾上腺嗜铬细胞中γ-氨基丁酸A型受体产生的兴奋作用中的作用
J Neurophysiol. 2003 Dec;90(6):3828-37. doi: 10.1152/jn.00617.2003. Epub 2003 Sep 10.
10
KCC2 function modulates in vitro ictogenesis.钾氯共转运体2（KCC2）的功能调节体外痫性发作的产生。
Neurobiol Dis. 2015 Jul;79:51-8. doi: 10.1016/j.nbd.2015.04.006. Epub 2015 Apr 26.

引用本文的文献

1
Combined use of CLP290 and bumetanide alleviates neuropathic pain and its mechanism after spinal cord injury in rats.CLP290 与布美他尼联合使用可缓解大鼠脊髓损伤后的神经病理性疼痛及其机制。
CNS Neurosci Ther. 2024 Sep;30(9):e70045. doi: 10.1111/cns.70045.
2
New epilepsy therapies in development.正在开发的新癫痫疗法。
Nat Rev Drug Discov. 2024 Sep;23(9):682-708. doi: 10.1038/s41573-024-00981-w. Epub 2024 Jul 22.
3
Compound 350: A New Hope for Individuals with Drug-resistant Epilepsy.化合物350：耐药性癫痫患者的新希望。
Ann Neurosci. 2024 Apr;31(2):80-82. doi: 10.1177/09727531231192758. Epub 2023 Nov 3.
4
: the implications of excitatory GABAergic signaling in neurological disorders.兴奋性γ-氨基丁酸能信号传导在神经疾病中的意义
Front Psychiatry. 2024 Jan 10;14:1296527. doi: 10.3389/fpsyt.2023.1296527. eCollection 2023.
5
The role of family of cation-chloride cotransporters and drug discovery methodologies.阳离子-氯离子共转运体家族的作用及药物发现方法
J Pharm Anal. 2023 Dec;13(12):1471-1495. doi: 10.1016/j.jpha.2023.09.002. Epub 2023 Sep 9.
6
Serine 937 phosphorylation enhances KCC2 activity and strengthens synaptic inhibition.丝氨酸 937 磷酸化增强 KCC2 活性并增强突触抑制。
Sci Rep. 2023 Dec 8;13(1):21660. doi: 10.1038/s41598-023-48884-x.
7
Neuronal K-Cl cotransporter KCC2 as a promising drug target for epilepsy treatment.神经元 K-Cl 协同转运蛋白 KCC2 作为治疗癫痫的有希望的药物靶点。
Acta Pharmacol Sin. 2024 Jan;45(1):1-22. doi: 10.1038/s41401-023-01149-9. Epub 2023 Sep 13.
8
KCC2 reverse mode helps to clear postsynaptically released potassium at glutamatergic synapses.KCC2 反向转运模式有助于清除谷氨酸能突触后释放的钾离子。
Cell Rep. 2023 Aug 29;42(8):112934. doi: 10.1016/j.celrep.2023.112934. Epub 2023 Aug 1.
9
Direct activation of KCC2 arrests benzodiazepine refractory status epilepticus and limits the subsequent neuronal injury in mice.直接激活 KCC2 可阻止苯二氮䓬类药物难治性癫痫持续状态，并限制随后在小鼠中的神经元损伤。
Cell Rep Med. 2023 Mar 21;4(3):100957. doi: 10.1016/j.xcrm.2023.100957. Epub 2023 Mar 7.
10
Structural Pharmacology of Cation-Chloride Cotransporters.阳离子-氯离子共转运体的结构药理学
Membranes (Basel). 2022 Nov 29;12(12):1206. doi: 10.3390/membranes12121206.

本文引用的文献

1
Seizing Control of KCC2: A New Therapeutic Target for Epilepsy.控制 KCC2：癫痫治疗的新靶点。
Trends Neurosci. 2017 Sep;40(9):555-571. doi: 10.1016/j.tins.2017.06.008. Epub 2017 Aug 10.
2
Enhancing KCC2 function counteracts morphine-induced hyperalgesia.增强 KCC2 功能可拮抗吗啡诱导的痛觉过敏。
Sci Rep. 2017 Jun 20;7(1):3870. doi: 10.1038/s41598-017-04209-3.
3
Stress Increases Ethanol Self-Administration via a Shift toward Excitatory GABA Signaling in the Ventral Tegmental Area.应激通过腹侧被盖区向兴奋性GABA信号的转变增加乙醇自我给药。
Neuron. 2016 Oct 19;92(2):493-504. doi: 10.1016/j.neuron.2016.09.029. Epub 2016 Oct 6.
4
Diminished KCC2 confounds synapse specificity of LTP during senescence.衰老过程中KCC2减少会混淆长时程增强的突触特异性。
Nat Neurosci. 2016 Sep;19(9):1197-200. doi: 10.1038/nn.4357. Epub 2016 Aug 8.
5
WNK1-regulated inhibitory phosphorylation of the KCC2 cotransporter maintains the depolarizing action of GABA in immature neurons.WNK1调节的KCC2共转运体抑制性磷酸化维持了未成熟神经元中GABA的去极化作用。
Sci Signal. 2015 Jun 30;8(383):ra65. doi: 10.1126/scisignal.aaa0354.
6
Selective inhibition of KCC2 leads to hyperexcitability and epileptiform discharges in hippocampal slices and in vivo.对KCC2的选择性抑制会导致海马切片和体内的兴奋性过高及癫痫样放电。
J Neurosci. 2015 May 27;35(21):8291-6. doi: 10.1523/JNEUROSCI.5205-14.2015.
7
KCC2 function modulates in vitro ictogenesis.钾氯共转运体2（KCC2）的功能调节体外痫性发作的产生。
Neurobiol Dis. 2015 Jul;79:51-8. doi: 10.1016/j.nbd.2015.04.006. Epub 2015 Apr 26.
8
Visualization of synaptic inhibition with an optogenetic sensor developed by cell-free protein engineering automation.利用无细胞蛋白工程自动化开发的光遗传传感器实现突触抑制可视化。
J Neurosci. 2013 Oct 9;33(41):16297-309. doi: 10.1523/JNEUROSCI.4616-11.2013.
9
Chloride extrusion enhancers as novel therapeutics for neurological diseases.氯离子外排增强剂：神经疾病治疗的新策略
Nat Med. 2013 Nov;19(11):1524-8. doi: 10.1038/nm.3356. Epub 2013 Oct 6.
10
Cystic fibrosis transmembrane regulator correctors and potentiators.囊性纤维化跨膜转导调节因子校正剂和增强剂。
Cold Spring Harb Perspect Med. 2013 Jul 1;3(7):a009761. doi: 10.1101/cshperspect.a009761.