• 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

倍半萜与甘氨酸-亮氨酸-丝氨酸/赖氨酸的“共适应口袋”结合以抑制肺癌细胞上皮-间质转化。

Sesquiterpene binding Gly-Leu-Ser/Lys-"co-adaptation pocket" to inhibit lung cancer cell epithelial-mesenchymal transition.

作者信息

Ai Xiao-Yu, Zhang Heng, Gao Shao-Yan, Qin Yuan, Zhong Wei-Long, Gu Ju, Li Meng, Qiao Kai-Liang, Tian Qin, Cui Zhan-Hong, Yang Jia-Huan, Bi Zhun, Xiao Ting, Chen Shuang, Liu Hui-Juan, Zhou Hong-Gang, Sun Tao, Yang Cheng

机构信息

State Key Laboratory of Medicinal Chemical Biology and College of Pharmacy, Nankai University, Tianjin, China.

Tianjin Key Laboratory of Molecular Drug Research, Tianjin International Joint Academy of Biomedicine, Tianjin, China.

出版信息

Oncotarget. 2017 Jul 26;8(41):70192-70203. doi: 10.18632/oncotarget.19599. eCollection 2017 Sep 19.

DOI:10.18632/oncotarget.19599
PMID:29050271
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5642546/
Abstract

Sesquiterpene lactones (SL) have a wide range of applications in anti-tumor and anti-inflammatory therapy. However, the pharmacological mechanism of such substances is not clear. In this study, parthenolide (PTL) was used as an example to explore the anti-tumor effect of natural molecules and their common mechanism. We showed that PTL inhibited the proliferation and migration by reverse EMT via the ERK2/NF-κB/Snail pathway and . Interestingly, Multiple potential targets of PTL contain a Gly-Leu-Ser/Lys-"co-adaptation pocket". This inspiring us analogies of PTL may also bind to these target proteins and play a similar function. Significantly, the Concept of co-adaptation pocket may help to increase the selectivity of drug research and development.

摘要

倍半萜内酯（SL）在抗肿瘤和抗炎治疗中有广泛应用。然而，这类物质的药理机制尚不清楚。在本研究中，以小白菊内酯（PTL）为例探讨天然分子的抗肿瘤作用及其共同机制。我们发现PTL通过ERK2/NF-κB/蜗牛蛋白途径逆转上皮-间质转化来抑制增殖和迁移。有趣的是，PTL的多个潜在靶点含有一个甘氨酸-亮氨酸-丝氨酸/赖氨酸“共适应口袋”。这启发我们，PTL的类似物可能也会与这些靶蛋白结合并发挥类似功能。值得注意的是，共适应口袋的概念可能有助于提高药物研发的选择性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f3/5642546/8192854079e5/oncotarget-08-70192-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f3/5642546/ce8649ae25c2/oncotarget-08-70192-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f3/5642546/69cfcc9091b9/oncotarget-08-70192-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f3/5642546/462a6c72be61/oncotarget-08-70192-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f3/5642546/ab3939d2f06e/oncotarget-08-70192-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f3/5642546/83373b690217/oncotarget-08-70192-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f3/5642546/8192854079e5/oncotarget-08-70192-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f3/5642546/ce8649ae25c2/oncotarget-08-70192-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f3/5642546/69cfcc9091b9/oncotarget-08-70192-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f3/5642546/462a6c72be61/oncotarget-08-70192-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f3/5642546/ab3939d2f06e/oncotarget-08-70192-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f3/5642546/83373b690217/oncotarget-08-70192-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f3/5642546/8192854079e5/oncotarget-08-70192-g006.jpg

相似文献

1
Sesquiterpene binding Gly-Leu-Ser/Lys-"co-adaptation pocket" to inhibit lung cancer cell epithelial-mesenchymal transition.倍半萜与甘氨酸-亮氨酸-丝氨酸/赖氨酸的“共适应口袋”结合以抑制肺癌细胞上皮-间质转化。
Oncotarget. 2017 Jul 26;8(41):70192-70203. doi: 10.18632/oncotarget.19599. eCollection 2017 Sep 19.
2
Inhibition of NF-kappaB by combination therapy with parthenolide and hyperthermia and kinetics of apoptosis induction and cell cycle arrest in human lung adenocarcinoma cells.联合使用小白菊内酯和热疗抑制 NF-κB 以及诱导人肺腺癌细胞凋亡和细胞周期停滞的动力学。
Int J Mol Med. 2010 Jan;25(1):81-7.
3
Lipocalin2 suppresses metastasis of colorectal cancer by attenuating NF-κB-dependent activation of snail and epithelial mesenchymal transition.脂质运载蛋白2通过减弱NF-κB依赖的蜗牛蛋白激活和上皮间质转化来抑制结直肠癌转移。
Mol Cancer. 2016 Dec 3;15(1):77. doi: 10.1186/s12943-016-0564-9.
4
The sesquiterpene lactone parthenolide induces selective apoptosis of B-chronic lymphocytic leukemia cells in vitro.倍半萜内酯小白菊内酯在体外可诱导B细胞慢性淋巴细胞白血病细胞发生选择性凋亡。
Leukemia. 2006 Jun;20(6):1073-9. doi: 10.1038/sj.leu.2404230.
5
Inhibition of epithelial to mesenchymal transition in metastatic prostate cancer cells by the novel proteasome inhibitor, NPI-0052: pivotal roles of Snail repression and RKIP induction.新型蛋白酶体抑制剂NPI-0052对转移性前列腺癌细胞上皮-间质转化的抑制作用：Snail抑制和RKIP诱导的关键作用
Oncogene. 2009 Oct 8;28(40):3573-85. doi: 10.1038/onc.2009.214. Epub 2009 Jul 27.
6
Thermosensitization by parthenolide in human lung adenocarcinoma A549 cells and p53- and hsp72-independent apoptosis induction via the nuclear factor-kappaB signal pathway.小白菊内酯对人肺腺癌A549细胞的热致敏作用及通过核因子-κB信号通路诱导不依赖p53和hsp72的细胞凋亡
Int J Mol Med. 2008 May;21(5):585-92.
7
Sesquiterpene lactones are potent inhibitors of interleukin 8 gene expression in cultured human respiratory epithelium.倍半萜内酯是培养的人呼吸道上皮中白细胞介素8基因表达的有效抑制剂。
Cytokine. 2000 Mar;12(3):239-45. doi: 10.1006/cyto.1999.0526.
8
Resveratrol suppresses epithelial-to-mesenchymal transition in colorectal cancer through TGF-β1/Smads signaling pathway mediated Snail/E-cadherin expression.白藜芦醇通过TGF-β1/Smads信号通路介导的Snail/E-钙黏蛋白表达抑制结直肠癌上皮-间质转化。
BMC Cancer. 2015 Mar 5;15:97. doi: 10.1186/s12885-015-1119-y.
9
Role of cysteine residues of p65/NF-kappaB on the inhibition by the sesquiterpene lactone parthenolide and N-ethyl maleimide, and on its transactivating potential.p65/NF-κB的半胱氨酸残基在倍半萜内酯小白菊内酯和N-乙基马来酰亚胺的抑制作用及其反式激活潜能方面的作用。
Life Sci. 2004 Jul 2;75(7):841-56. doi: 10.1016/j.lfs.2004.01.024.
10
Stereospecific effects of ginsenoside 20-Rg3 inhibits TGF-β1-induced epithelial-mesenchymal transition and suppresses lung cancer migration, invasion and anoikis resistance.人参皂苷20-Rg3的立体特异性作用抑制TGF-β1诱导的上皮-间质转化并抑制肺癌的迁移、侵袭和失巢凋亡抗性。
Toxicology. 2014 Aug 1;322:23-33. doi: 10.1016/j.tox.2014.04.002. Epub 2014 May 2.

引用本文的文献

1
The Emerging Potential of Parthenolide Nanoformulations in Tumor Therapy.姜烯酮纳米制剂在肿瘤治疗中的新兴潜力。
Drug Des Devel Ther. 2022 Apr 29;16:1255-1272. doi: 10.2147/DDDT.S355059. eCollection 2022.
2
Reversal of Epithelial-Mesenchymal Transition by Natural Anti-Inflammatory and Pro-Resolving Lipids.天然抗炎及促消退脂质逆转上皮-间质转化
Cancers (Basel). 2019 Nov 21;11(12):1841. doi: 10.3390/cancers11121841.

本文引用的文献

1
Redundancy in the World of MAP Kinases: All for One.MAP 激酶世界中的冗余：一荣俱荣。
Front Cell Dev Biol. 2016 Jun 27;4:67. doi: 10.3389/fcell.2016.00067. eCollection 2016.
2
ERK1 and ERK2 Map Kinases: Specific Roles or Functional Redundancy?ERK1 和 ERK2 丝裂原活化蛋白激酶：特定作用还是功能冗余？
Front Cell Dev Biol. 2016 Jun 8;4:53. doi: 10.3389/fcell.2016.00053. eCollection 2016.
3
Apigenin inhibits NF-κB and snail signaling, EMT and metastasis in human hepatocellular carcinoma.芹菜素抑制人肝细胞癌中的核因子κB和蜗牛信号通路、上皮-间质转化及转移。
Oncotarget. 2016 Jul 5;7(27):41421-41431. doi: 10.18632/oncotarget.9404.
4
Doxycycline reverses epithelial-to-mesenchymal transition and suppresses the proliferation and metastasis of lung cancer cells.强力霉素可逆转上皮-间质转化并抑制肺癌细胞的增殖和转移。
Oncotarget. 2015 Dec 1;6(38):40667-79. doi: 10.18632/oncotarget.5842.
5
DKK3 blocked translocation of β-catenin/EMT induced by hypoxia and improved gemcitabine therapeutic effect in pancreatic cancer Bxpc-3 cell.DKK3可阻断缺氧诱导的β-连环蛋白/上皮-间质转化（EMT）易位，并提高吉西他滨对胰腺癌Bxpc-3细胞的治疗效果。
J Cell Mol Med. 2015 Dec;19(12):2832-41. doi: 10.1111/jcmm.12675. Epub 2015 Sep 23.
6
Balsalazide Potentiates Parthenolide-Mediated Inhibition of Nuclear Factor-κB Signaling in HCT116 Human Colorectal Cancer Cells.巴柳氮增强小白菊内酯介导的对HCT116人结肠癌细胞中核因子-κB信号传导的抑制作用。
Intest Res. 2015 Jul;13(3):233-41. doi: 10.5217/ir.2015.13.3.233. Epub 2015 Jun 9.
7
Parthenolide Relieves Pain and Promotes M2 Microglia/Macrophage Polarization in Rat Model of Neuropathy.小白菊内酯缓解大鼠神经病变模型中的疼痛并促进M2小胶质细胞/巨噬细胞极化。
Neural Plast. 2015;2015:676473. doi: 10.1155/2015/676473. Epub 2015 May 18.
8
Suppression of tubulin detyrosination by parthenolide recruits the plant-specific kinesin KCH to cortical microtubules.小白菊内酯对微管蛋白去酪氨酸化的抑制作用促使植物特异性驱动蛋白KCH定位于皮层微管。
J Exp Bot. 2015 Apr;66(7):2001-11. doi: 10.1093/jxb/erv012. Epub 2015 Mar 16.
9
Parthenolide inhibits pro-inflammatory cytokine production and exhibits protective effects on progression of collagen-induced arthritis in a rat model.小白菊内酯可抑制促炎细胞因子的产生，并对大鼠胶原诱导性关节炎的进展具有保护作用。
Scand J Rheumatol. 2015 May;44(3):182-91. doi: 10.3109/03009742.2014.938113. Epub 2014 Dec 2.
10
Micheliolide, a new sesquiterpene lactone that inhibits intestinal inflammation and colitis-associated cancer.米契罗内酯，一种抑制肠道炎症和结肠炎相关癌症的新型倍半萜内酯。
Lab Invest. 2014 Sep;94(9):950-65. doi: 10.1038/labinvest.2014.89. Epub 2014 Jul 28.