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Disruption of transcriptionally active Stat3 dimers with non-phosphorylated, salicylic acid-based small molecules: potent in vitro and tumor cell activities.用基于水杨酸的非磷酸化小分子破坏转录活性Stat3二聚体：强大的体外和肿瘤细胞活性。
Chembiochem. 2009 Aug 17;10(12):1959-64. doi: 10.1002/cbic.200900172.
2
Identification of a non-phosphorylated, cell permeable, small molecule ligand for the Stat3 SH2 domain.鉴定 Stat3 SH2 结构域的非磷酸化、细胞通透的小分子配体。
Bioorg Med Chem Lett. 2011 Sep 15;21(18):5605-9. doi: 10.1016/j.bmcl.2011.06.056. Epub 2011 Jun 30.
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Antagonism of the Stat3-Stat3 protein dimer with salicylic acid based small molecules.用基于水杨酸的小分子拮抗 Stat3-Stat3 二聚体。
ChemMedChem. 2011 Aug 1;6(8):1459-70. doi: 10.1002/cmdc.201100194. Epub 2011 May 25.
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Combined STAT3 and BCR-ABL1 inhibition induces synthetic lethality in therapy-resistant chronic myeloid leukemia.联合抑制信号转导与转录激活因子3（STAT3）和断裂簇区域蛋白-阿贝尔逊鼠白血病病毒1（BCR-ABL1）可在耐药性慢性髓性白血病中诱导合成致死效应。
Leukemia. 2015 Mar;29(3):586-597. doi: 10.1038/leu.2014.245. Epub 2014 Aug 19.
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Micellar nano-carriers for the delivery of STAT3 dimerization inhibitors to melanoma.用于将 STAT3 二聚化抑制剂递送至黑色素瘤的胶束纳米载体。
Drug Deliv Transl Res. 2017 Aug;7(4):571-581. doi: 10.1007/s13346-017-0369-4.
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Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity.通过基于结构的虚拟筛选鉴定出的Stat3选择性化学探针抑制剂可诱导抗肿瘤活性。
Proc Natl Acad Sci U S A. 2007 May 1;104(18):7391-6. doi: 10.1073/pnas.0609757104. Epub 2007 Apr 26.
7
Changes in signal transducer and activator of transcription 3 (STAT3) dynamics induced by complexation with pharmacological inhibitors of Src homology 2 (SH2) domain dimerization.与Src同源2（SH2）结构域二聚化的药理抑制剂复合所诱导的信号转导和转录激活因子3（STAT3）动力学变化。
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A novel small-molecule disrupts Stat3 SH2 domain-phosphotyrosine interactions and Stat3-dependent tumor processes.一种新型小分子破坏 Stat3 SH2 结构域-磷酸酪氨酸相互作用和 Stat3 依赖性肿瘤过程。
Biochem Pharmacol. 2010 May 15;79(10):1398-409. doi: 10.1016/j.bcp.2010.01.001. Epub 2010 Jan 11.

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Design, synthesis, and anti-hepatocellular carcinoma of thiopyrimidine/chalcone hybrids as dual STAT3/STAT5 inhibitors.作为双STAT3/STAT5抑制剂的硫代嘧啶/查尔酮杂合物的设计、合成及抗肝细胞癌活性
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Decoding IL-23 Signaling Cascade for New Therapeutic Opportunities.解析 IL-23 信号级联反应，寻找新的治疗机会。
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Cancers (Basel). 2020 Aug 30;12(9):2459. doi: 10.3390/cancers12092459.
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Pharmacological Inhibition of Oncogenic STAT3 and STAT5 Signaling in Hematopoietic Cancers.造血系统癌症中致癌性 STAT3 和 STAT5 信号通路的药理学抑制作用
Cancers (Basel). 2020 Jan 18;12(1):240. doi: 10.3390/cancers12010240.
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Direct Targeting Options for STAT3 and STAT5 in Cancer.癌症中STAT3和STAT5的直接靶向治疗选择
Cancers (Basel). 2019 Dec 3;11(12):1930. doi: 10.3390/cancers11121930.
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Natural Sesquiterpene Lactones Enhance Chemosensitivity of Tumor Cells through Redox Regulation of STAT3 Signaling.天然倍半萜内酯通过调节 STAT3 信号的氧化还原状态增强肿瘤细胞的化疗敏感性。
Oxid Med Cell Longev. 2019 Oct 28;2019:4568964. doi: 10.1155/2019/4568964. eCollection 2019.
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Phosphotyrosine isosteres: past, present and future.磷酸酪氨酸类似物：过去、现在和未来。
Org Biomol Chem. 2020 Jan 28;18(4):583-605. doi: 10.1039/c9ob01998g. Epub 2019 Nov 28.

本文引用的文献

1
Inhibition of the sodium potassium adenosine triphosphatase pump sensitizes cancer cells to anoikis and prevents distant tumor formation.抑制钠钾三磷酸腺苷酶泵可使癌细胞对失巢凋亡敏感，并防止远处肿瘤形成。
Cancer Res. 2009 Apr 1;69(7):2739-47. doi: 10.1158/0008-5472.CAN-08-2530. Epub 2009 Mar 17.
2
Targeting STAT3 in cancer: how successful are we?在癌症中靶向 STAT3：我们有多成功？
Expert Opin Investig Drugs. 2009 Jan;18(1):45-56. doi: 10.1517/13543780802565791.
3
Targeting protein-protein interactions: suppression of Stat3 dimerization with rationally designed small-molecule, nonpeptidic SH2 domain binders.靶向蛋白质-蛋白质相互作用：用合理设计的小分子非肽类SH2结构域结合剂抑制Stat3二聚化
Chembiochem. 2008 Nov 24;9(17):2800-3. doi: 10.1002/cbic.200800291.
4
Molecular approaches towards the inhibition of the signal transducer and activator of transcription 3 (Stat3) protein.抑制信号转导与转录激活因子3（Stat3）蛋白的分子方法。
ChemMedChem. 2008 Aug;3(8):1159-68. doi: 10.1002/cmdc.200800123.
5
Signal transducers and activators of transcription as targets for small organic molecules.作为小分子有机化合物作用靶点的信号转导及转录激活因子
Chembiochem. 2008 Sep 1;9(13):2039-44. doi: 10.1002/cbic.200800274.
6
An oxazole-based small-molecule Stat3 inhibitor modulates Stat3 stability and processing and induces antitumor cell effects.一种基于恶唑的小分子信号转导和转录激活因子3（Stat3）抑制剂可调节Stat3的稳定性和加工过程，并诱导抗肿瘤细胞效应。
ACS Chem Biol. 2007 Dec 21;2(12):787-98. doi: 10.1021/cb7001973.
7
Stat3 is tyrosine-phosphorylated through the interleukin-6/glycoprotein 130/Janus kinase pathway in breast cancer.在乳腺癌中，信号转导与转录激活因子3（Stat3）通过白细胞介素-6/糖蛋白130/Janus激酶途径发生酪氨酸磷酸化。
Breast Cancer Res. 2007;9(3):R32. doi: 10.1186/bcr1680.
8
Design and synthesis of a new, conformationally constrained, macrocyclic small-molecule inhibitor of STAT3 via 'click chemistry'.通过“点击化学”设计并合成一种新型的、构象受限的STAT3大环小分子抑制剂。
Bioorg Med Chem Lett. 2007 Jul 15;17(14):3939-42. doi: 10.1016/j.bmcl.2007.04.096. Epub 2007 May 3.
9
New syntheses of tetrazolylmethylphenylalanine and O-malonyltyrosine as pTyr mimetics for the design of STAT3 dimerization inhibitors.作为用于设计STAT3二聚化抑制剂的对酪氨酸（pTyr）模拟物的四唑基甲基苯丙氨酸和O-丙二酰酪氨酸的新合成方法。
Bioorg Med Chem Lett. 2007 Jul 15;17(14):3943-6. doi: 10.1016/j.bmcl.2007.04.107. Epub 2007 May 3.
10
Protein-protein interaction inhibitors: small molecules from screening techniques.蛋白质-蛋白质相互作用抑制剂：来自筛选技术的小分子
Curr Top Med Chem. 2007;7(10):922-7. doi: 10.2174/156802607780906735.

Disruption of transcriptionally active Stat3 dimers with non-phosphorylated, salicylic acid-based small molecules: potent in vitro and tumor cell activities.

作者信息

Fletcher Steven, Singh Jagdeep, Zhang Xiaolei, Yue Peibin, Page Brent D G, Sharmeen Sumaiya, Shahani Vijay M, Zhao Wei, Schimmer Aaron D, Turkson James, Gunning Patrick T

机构信息

Department of Chemistry, University of Toronto, Mississauga, Mississauga, ON L5L 1C6 (Canada).

出版信息

Chembiochem. 2009 Aug 17;10(12):1959-64. doi: 10.1002/cbic.200900172.

DOI:10.1002/cbic.200900172
PMID:19644994
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2919050/
Abstract
摘要