• 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

达沙替尼通过抑制尼罗替尼耐药慢性髓性白血病细胞系中的 Lyn 激酶,优先诱导细胞凋亡。

Dasatinib preferentially induces apoptosis by inhibiting Lyn kinase in nilotinib-resistant chronic myeloid leukemia cell line.

出版信息

J Hematol Oncol. 2011 Aug 2;4(1):32. doi: 10.1186/1756-8722-4-32.

DOI:10.1186/1756-8722-4-32
PMID:21806844
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3163636/
Abstract

Nilotinib is approved for treatment of newly diagnosed chronic myeloid leukemia (CML) and it is shown superiority over imatinib in first-line treatment for patients of CML. In this study, we established a nilotinib-resistant cell line, K562NR, and evaluated the resistance to nilotinib and efficacy of dasatinib. We found activation of Lyn plays a dominant role in survival of the nilotinib-resistant cell line. We found dasatinib induces the apoptosis of nilotinib-resistant cells and inhibits Lyn kinase activity. This novel nilotinib-resistant CML cell line may help to explore novel therapy for CML.

摘要

尼洛替尼已被批准用于治疗新诊断的慢性髓性白血病(CML),并且在 CML 患者的一线治疗中显示出优于伊马替尼的优势。在这项研究中,我们建立了尼洛替尼耐药细胞系 K562NR,并评估了对尼洛替尼的耐药性和达沙替尼的疗效。我们发现 Lyn 的激活在尼洛替尼耐药细胞系的存活中起主导作用。我们发现达沙替尼诱导尼洛替尼耐药细胞凋亡并抑制 Lyn 激酶活性。这种新型尼洛替尼耐药 CML 细胞系可能有助于探索 CML 的新治疗方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efda/3163636/e4bd6504ac47/1756-8722-4-32-1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efda/3163636/e4bd6504ac47/1756-8722-4-32-1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efda/3163636/e4bd6504ac47/1756-8722-4-32-1.jpg

相似文献

1
Dasatinib preferentially induces apoptosis by inhibiting Lyn kinase in nilotinib-resistant chronic myeloid leukemia cell line.达沙替尼通过抑制尼罗替尼耐药慢性髓性白血病细胞系中的 Lyn 激酶,优先诱导细胞凋亡。
J Hematol Oncol. 2011 Aug 2;4(1):32. doi: 10.1186/1756-8722-4-32.
2
Evidence that resistance to nilotinib may be due to BCR-ABL, Pgp, or Src kinase overexpression.对尼罗替尼产生耐药性可能归因于BCR-ABL、Pgp或Src激酶过表达的证据。
Cancer Res. 2008 Dec 1;68(23):9809-16. doi: 10.1158/0008-5472.CAN-08-1008.
3
Cotreatment with vorinostat (suberoylanilide hydroxamic acid) enhances activity of dasatinib (BMS-354825) against imatinib mesylate-sensitive or imatinib mesylate-resistant chronic myelogenous leukemia cells.伏立诺他(辛二酰苯胺异羟肟酸)与达沙替尼(BMS-354825)联合治疗可增强达沙替尼对甲磺酸伊马替尼敏感或甲磺酸伊马替尼耐药的慢性粒细胞白血病细胞的活性。
Clin Cancer Res. 2006 Oct 1;12(19):5869-78. doi: 10.1158/1078-0432.CCR-06-0980.
4
Dasatinib (BMS-354825) inhibits Stat5 signaling associated with apoptosis in chronic myelogenous leukemia cells.达沙替尼(BMS-354825)抑制慢性粒细胞白血病细胞中与凋亡相关的Stat5信号传导。
Mol Cancer Ther. 2007 Apr;6(4):1400-5. doi: 10.1158/1535-7163.MCT-06-0446.
5
Expression of LYN and PTEN genes in chronic myeloid leukemia and their importance in therapeutic strategy.LYN 和 PTEN 基因在慢性髓性白血病中的表达及其在治疗策略中的重要性。
Blood Cells Mol Dis. 2014 Feb-Mar;52(2-3):121-5. doi: 10.1016/j.bcmd.2013.09.002. Epub 2013 Oct 3.
6
Effects of dasatinib on SRC kinase activity and downstream intracellular signaling in primitive chronic myelogenous leukemia hematopoietic cells.达沙替尼对原始慢性粒细胞白血病造血细胞中SRC激酶活性及下游细胞内信号传导的影响。
Cancer Res. 2008 Dec 1;68(23):9624-33. doi: 10.1158/0008-5472.CAN-08-1131.
7
MEK1/2 inhibitors sensitize Bcr/Abl+ human leukemia cells to the dual Abl/Src inhibitor BMS-354/825.MEK1/2抑制剂使Bcr/Abl+人白血病细胞对双重Abl/Src抑制剂BMS-354/825敏感。
Blood. 2007 May 1;109(9):4006-15. doi: 10.1182/blood-2006-09-045039. Epub 2007 Jan 11.
8
Overcoming imatinib resistance using Src inhibitor CGP76030, Abl inhibitor nilotinib and Abl/Lyn inhibitor INNO-406 in newly established K562 variants with BCR-ABL gene amplification.在新建立的具有BCR-ABL基因扩增的K562变体中,使用Src抑制剂CGP76030、Abl抑制剂尼罗替尼和Abl/Lyn抑制剂INNO-406克服伊马替尼耐药性。
Int J Cancer. 2008 Jun 1;122(11):2621-7. doi: 10.1002/ijc.23435.
9
Inhibition of imatinib-mediated apoptosis by the caspase-cleaved form of the tyrosine kinase Lyn in chronic myelogenous leukemia cells.在慢性粒细胞白血病细胞中,酪氨酸激酶Lyn的半胱天冬酶切割形式对伊马替尼介导的细胞凋亡的抑制作用。
Leukemia. 2009 Aug;23(8):1500-6. doi: 10.1038/leu.2009.60. Epub 2009 Apr 2.
10
Chemical proteomic profiles of the BCR-ABL inhibitors imatinib, nilotinib, and dasatinib reveal novel kinase and nonkinase targets.BCR-ABL抑制剂伊马替尼、尼洛替尼和达沙替尼的化学蛋白质组学图谱揭示了新的激酶和非激酶靶点。
Blood. 2007 Dec 1;110(12):4055-63. doi: 10.1182/blood-2007-07-102061. Epub 2007 Aug 24.

引用本文的文献

1
Antisenescence Therapy Improves Function in a Human Model of Cardiac Fibrosis-on-a-Chip.抗衰老疗法改善了芯片上心脏纤维化人类模型的功能。
ACS Mater Au. 2023 May 2;3(4):360-370. doi: 10.1021/acsmaterialsau.3c00009. eCollection 2023 Jul 12.
2
Methods for Design of Kinase Inhibitors as Anticancer Drugs.激酶抑制剂作为抗癌药物的设计方法。
Front Chem. 2020 Jan 8;7:873. doi: 10.3389/fchem.2019.00873. eCollection 2019.
3
Effect of dual inhibition of histone deacetylase and phosphatidylinositol-3 kinase in Philadelphia chromosome-positive leukemia cells.

本文引用的文献

1
BCR-ABL1-independent PI3Kinase activation causing imatinib-resistance.BCR-ABL1 非依赖性 PI3K 激活导致伊马替尼耐药。
J Hematol Oncol. 2011 Feb 7;4:6. doi: 10.1186/1756-8722-4-6.
2
First-line treatment for chronic myeloid leukemia: dasatinib, nilotinib, or imatinib.慢性髓性白血病的一线治疗:达沙替尼、尼洛替尼或伊马替尼。
J Hematol Oncol. 2010 Nov 26;3:47. doi: 10.1186/1756-8722-3-47.
3
Dasatinib versus imatinib in newly diagnosed chronic-phase chronic myeloid leukemia.达沙替尼与伊马替尼治疗新诊断的慢性期慢性髓性白血病。
双重抑制组蛋白去乙酰化酶和磷酸肌醇-3 激酶对费城染色体阳性白血病细胞的影响。
Cancer Chemother Pharmacol. 2020 Feb;85(2):401-412. doi: 10.1007/s00280-019-04022-x. Epub 2020 Jan 4.
4
The Importance of the Right Framework: Mitogen-Activated Protein Kinase Pathway and the Scaffolding Protein PTPIP51.正确框架的重要性:丝裂原活化蛋白激酶途径和支架蛋白 PTPIP51。
Int J Mol Sci. 2018 Oct 22;19(10):3282. doi: 10.3390/ijms19103282.
5
Therapeutic targeting of Aurora A kinase in Philadelphia chromosome-positive ABL tyrosine kinase inhibitor-resistant cells.在费城染色体阳性的ABL酪氨酸激酶抑制剂耐药细胞中对极光激酶A进行治疗性靶向作用。
Oncotarget. 2018 Aug 21;9(65):32496-32506. doi: 10.18632/oncotarget.25985.
6
Lyn mediates FIP1L1-PDGFRA signal pathway facilitating IL-5RA intracellular signal through FIP1L1-PDGFRA/JAK2/Lyn/Akt network complex in CEL.Lyn介导FIP1L1-PDGFRA信号通路,通过FIP1L1-PDGFRA/JAK2/Lyn/Akt网络复合体促进嗜酸性粒细胞增多综合征中IL-5RA的细胞内信号传导。
Oncotarget. 2016 Aug 19;8(39):64984-64998. doi: 10.18632/oncotarget.11401. eCollection 2017 Sep 12.
7
A Cell-Based Assay for Measuring Endogenous BcrAbl Kinase Activity and Inhibitor Resistance.一种基于细胞的测定内源性BcrAbl激酶活性及抑制剂耐药性的方法。
PLoS One. 2016 Sep 6;11(9):e0161748. doi: 10.1371/journal.pone.0161748. eCollection 2016.
8
ABCB1 Overexpression Is a Key Initiator of Resistance to Tyrosine Kinase Inhibitors in CML Cell Lines.ABCB1过表达是慢性粒细胞白血病细胞系对酪氨酸激酶抑制剂耐药的关键启动因素。
PLoS One. 2016 Aug 18;11(8):e0161470. doi: 10.1371/journal.pone.0161470. eCollection 2016.
9
Dasatinib-loaded albumin nanoparticles possess diminished endothelial cell barrier disruption and retain potent anti-leukemia cell activity.负载达沙替尼的白蛋白纳米颗粒具有减少的内皮细胞屏障破坏作用,并保留强大的抗白血病细胞活性。
Oncotarget. 2016 Aug 2;7(31):49699-49709. doi: 10.18632/oncotarget.10435.
10
Distinct Dasatinib-Induced Mechanisms of Apoptotic Response and Exosome Release in Imatinib-Resistant Human Chronic Myeloid Leukemia Cells.达沙替尼诱导伊马替尼耐药的人慢性髓性白血病细胞凋亡反应和外泌体释放的不同机制。
Int J Mol Sci. 2016 Apr 8;17(4):531. doi: 10.3390/ijms17040531.
N Engl J Med. 2010 Jun 17;362(24):2260-70. doi: 10.1056/NEJMoa1002315. Epub 2010 Jun 5.
4
Nilotinib versus imatinib for newly diagnosed chronic myeloid leukemia.尼洛替尼与伊马替尼用于治疗新诊断的慢性髓性白血病。
N Engl J Med. 2010 Jun 17;362(24):2251-9. doi: 10.1056/NEJMoa0912614. Epub 2010 Jun 5.
5
New insights into the pathophysiology of chronic myeloid leukemia and imatinib resistance.慢性髓性白血病的病理生理学及伊马替尼耐药性的新见解。
Ann Intern Med. 2006 Dec 19;145(12):913-23. doi: 10.7326/0003-4819-145-12-200612190-00008.
6
Dasatinib (BMS-354825) is active in Philadelphia chromosome-positive chronic myelogenous leukemia after imatinib and nilotinib (AMN107) therapy failure.达沙替尼(BMS-354825)在伊马替尼和尼罗替尼(AMN107)治疗失败后的费城染色体阳性慢性髓性白血病中具有活性。
Blood. 2007 Jan 15;109(2):497-9. doi: 10.1182/blood-2006-07-035493. Epub 2006 Sep 21.
7
Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL.尼洛替尼用于伊马替尼耐药的慢性粒细胞白血病和费城染色体阳性的急性淋巴细胞白血病。
N Engl J Med. 2006 Jun 15;354(24):2542-51. doi: 10.1056/NEJMoa055104.
8
The development of imatinib as a therapeutic agent for chronic myeloid leukemia.伊马替尼作为慢性髓性白血病治疗药物的研发。
Blood. 2005 Apr 1;105(7):2640-53. doi: 10.1182/blood-2004-08-3097. Epub 2004 Dec 23.
9
Lyn is required for normal stem cell factor-induced proliferation and chemotaxis of primary hematopoietic cells.Lyn是原代造血细胞正常的干细胞因子诱导增殖和趋化所必需的。
Blood. 2001 Jul 15;98(2):343-50. doi: 10.1182/blood.v98.2.343.