• 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

选择性蛋白激酶C抑制剂GF 109203X可抑制佛波酯诱导的SH-SY5Y人神经母细胞瘤细胞的形态和功能分化。

The selective protein kinase C inhibitor GF 109203X inhibits phorbol ester-induced morphological and functional differentiation of SH-SY5Y human neuroblastoma cells.

作者信息

Heikkilä J, Jalava A, Eriksson K

机构信息

Department of Biochemistry and Pharmacy, Abo Akademi University, BioCity, Turku, Finland.

出版信息

Biochem Biophys Res Commun. 1993 Dec 30;197(3):1185-93. doi: 10.1006/bbrc.1993.2602.

DOI:10.1006/bbrc.1993.2602
PMID:8280132
Abstract

Previous attempts to inhibit the phorbol ester 12-O-tetradecanoyl phorbol 13-acetate (TPA) -induced differentiation of SH-SY5Y neuroblastoma cells by non-specific inhibitors of protein kinases have failed. In the present study we have used the bisindolylmaleimide GF 109203X, which is a potent and selective inhibitor of protein kinase C (PKC). GF 109203X effectively antagonized TPA-stimulated phosphorylation of an endogenous 80 kDa PKC substrate. The compound blocked neurite outgrowth and rounding up of cells induced by the phorbol ester. In addition, GF 109203X completely inhibited TPA-induced increase in cellular content of noradrenaline as well as stimulation of expression of neuropeptide Y, growth-associated protein-43 and c-fos proto-oncogene mRNA by TPA. The inhibition of the TPA-induced effects by GF 109203X was dose-dependent.

摘要

以往试图通过蛋白激酶非特异性抑制剂来抑制佛波酯12 - O -十四烷酰佛波醇13 - 乙酸酯（TPA）诱导的SH - SY5Y神经母细胞瘤细胞分化的尝试均告失败。在本研究中，我们使用了双吲哚马来酰胺GF 109203X，它是蛋白激酶C（PKC）的一种强效且选择性的抑制剂。GF 109203X有效拮抗了TPA刺激的内源性80 kDa PKC底物的磷酸化。该化合物阻断了佛波酯诱导的神经突生长和细胞变圆。此外，GF 109203X完全抑制了TPA诱导的去甲肾上腺素细胞含量增加以及TPA对神经肽Y、生长相关蛋白 - 43和c - fos原癌基因mRNA表达的刺激。GF 109203X对TPA诱导效应的抑制呈剂量依赖性。

相似文献

1
The selective protein kinase C inhibitor GF 109203X inhibits phorbol ester-induced morphological and functional differentiation of SH-SY5Y human neuroblastoma cells.选择性蛋白激酶C抑制剂GF 109203X可抑制佛波酯诱导的SH-SY5Y人神经母细胞瘤细胞的形态和功能分化。
Biochem Biophys Res Commun. 1993 Dec 30;197(3):1185-93. doi: 10.1006/bbrc.1993.2602.
2
Protein kinase C-epsilon is implicated in neurite outgrowth in differentiating human neuroblastoma cells.蛋白激酶C-ε与分化中的人神经母细胞瘤细胞的神经突生长有关。
Cell Growth Differ. 1996 Jun;7(6):775-85.
3
Protein kinase inhibitor, staurosporine, induces a mature neuronal phenotype in SH-SY5Y human neuroblastoma cells through an alpha-, beta-, and zeta-protein kinase C-independent pathway.蛋白激酶抑制剂星形孢菌素通过一条不依赖α、β和ζ蛋白激酶C的途径，诱导人神经母细胞瘤SH-SY5Y细胞形成成熟神经元表型。
J Cell Physiol. 1993 May;155(2):301-12. doi: 10.1002/jcp.1041550211.
4
Differential modulation of human fibroblast and keratinocyte growth by the protein kinase C inhibitor GF 109203X.
Mol Pharmacol. 1994 Sep;46(3):445-51.
5
Staurosporine induces a neuronal phenotype in SH-SY5Y human neuroblastoma cells that resembles that induced by the phorbol ester 12-O-tetradecanoyl phorbol-13 acetate (TPA).
FEBS Lett. 1992 Mar 30;300(2):114-8. doi: 10.1016/0014-5793(92)80176-h.
6
Protein kinase C-dependent tyrosine phosphorylation of p130cas in differentiating neuroblastoma cells.分化中的神经母细胞瘤细胞中p130cas的蛋白激酶C依赖性酪氨酸磷酸化
J Biol Chem. 1998 Jan 23;273(4):2336-43. doi: 10.1074/jbc.273.4.2336.
7
Fos and Jun form cell specific protein complexes at the neuropeptide tyrosine promoter.Fos和Jun在神经肽酪氨酸启动子处形成细胞特异性蛋白复合物。
Oncogene. 1994 Aug;9(8):2369-75.
8
A functional role for ERK in gene induction, but not in neurite outgrowth in differentiating neuroblastoma cells.
Exp Cell Res. 2001 Apr 15;265(1):21-30. doi: 10.1006/excr.2001.5163.
9
Effects of the selective bisindolylmaleimide protein kinase C inhibitor GF 109203X on P-glycoprotein-mediated multidrug resistance.选择性双吲哚马来酰亚胺蛋白激酶C抑制剂GF 109203X对P-糖蛋白介导的多药耐药性的影响
Br J Cancer. 1996 Sep;74(6):897-905. doi: 10.1038/bjc.1996.454.
10
PMA inhibits the growth of human fibroblasts after the induction of immediate-early genes.佛波酯在诱导即早基因后可抑制人成纤维细胞的生长。
Exp Cell Res. 1994 May;212(1):105-12. doi: 10.1006/excr.1994.1124.

引用本文的文献

1
Investigating the Role of Guanosine on Human Neuroblastoma Cell Differentiation and the Underlying Molecular Mechanisms.探究鸟苷对人神经母细胞瘤细胞分化的作用及其潜在分子机制。
Front Pharmacol. 2021 Apr 27;12:658806. doi: 10.3389/fphar.2021.658806. eCollection 2021.
2
Combined cisplatin and aurora inhibitor treatment increase neuroblastoma cell death but surviving cells overproduce BDNF.联合顺铂和 Aurora 抑制剂治疗可增加神经母细胞瘤细胞死亡，但存活细胞过度产生 BDNF。
Biol Open. 2016 Jul 15;5(7):899-907. doi: 10.1242/bio.016725.
3
Staurosporine synergistically potentiates the deoxycholate-mediated induction of COX-2 expression.
星形孢菌素协同增强脱氧胆酸盐介导的COX - 2表达诱导作用。
Physiol Rep. 2014 Aug 28;2(8). doi: 10.14814/phy2.12143. Print 2014 Aug 1.
4
Building bridges toward invasion: tumor promoter treatment induces a novel protein kinase C-dependent phenotype in MCF10A mammary cell acini.搭建侵袭之桥：肿瘤促进剂处理诱导MCF10A乳腺细胞腺泡中一种新的蛋白激酶C依赖性表型。
PLoS One. 2014 Mar 5;9(3):e90722. doi: 10.1371/journal.pone.0090722. eCollection 2014.
5
Multiple protein kinases determine the phosphorylated state of the small heat shock protein, HSP27, in SH-SY5Y neuroblastoma cells.多种蛋白激酶决定 SH-SY5Y 神经母细胞瘤细胞中小热休克蛋白 HSP27 的磷酸化状态。
Neuropharmacology. 2011 Jul-Aug;61(1-2):12-24. doi: 10.1016/j.neuropharm.2011.02.010. Epub 2011 Feb 19.
6
Novel PKCs activate ERK through PKD1 in MCF-7 cells.新型蛋白激酶 C 通过 PKD1 在 MCF-7 细胞中激活 ERK。
In Vitro Cell Dev Biol Anim. 2011 Jan;47(1):73-81. doi: 10.1007/s11626-010-9355-6. Epub 2010 Nov 13.
7
Phorbol ester phorbol-12-myristate-13-acetate induces epithelial to mesenchymal transition in human prostate cancer ARCaPE cells.佛波酯 12-肉豆蔻酸-13-乙酸酯诱导人前列腺癌细胞系 ARCaPE 上皮间质转化。
Prostate. 2010 Jul 1;70(10):1119-26. doi: 10.1002/pros.21146.
8
Urocortin, but not urocortin II, protects cultured hippocampal neurons from oxidative and excitotoxic cell death via corticotropin-releasing hormone receptor type I.尿皮质素而非尿皮质素II，通过I型促肾上腺皮质激素释放激素受体保护培养的海马神经元免受氧化和兴奋性毒性细胞死亡。
J Neurosci. 2002 Jan 15;22(2):404-12. doi: 10.1523/JNEUROSCI.22-02-00404.2002.
9
p21WAF1 expression by an activator of protein kinase C is regulated mainly at the post-transcriptional level in cells lacking p53: important role of RNA stabilization.蛋白激酶C激活剂介导的p21WAF1表达在缺乏p53的细胞中主要在转录后水平受到调控：RNA稳定的重要作用。
Biochem J. 1999 Feb 1;337 ( Pt 3)(Pt 3):607-16.
10
Effects of the selective bisindolylmaleimide protein kinase C inhibitor GF 109203X on P-glycoprotein-mediated multidrug resistance.选择性双吲哚马来酰亚胺蛋白激酶C抑制剂GF 109203X对P-糖蛋白介导的多药耐药性的影响
Br J Cancer. 1996 Sep;74(6):897-905. doi: 10.1038/bjc.1996.454.