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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.
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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。
J Biol Chem. 2014 Nov 21;289(47):32538-47. doi: 10.1074/jbc.M114.595454. Epub 2014 Oct 6.
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A novel non-phosphorylated potential antitumoral peptide inhibits STAT3 biological activity.一种新型非磷酸化潜在抗肿瘤肽可抑制信号转导和转录激活因子3（STAT3）的生物学活性。
Biochimie. 2009 Aug;91(8):996-1002. doi: 10.1016/j.biochi.2009.05.006. Epub 2009 May 24.
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Discovery of novel STAT3 small molecule inhibitors via in silico site-directed fragment-based drug design.通过基于计算机的定向片段药物设计发现新型 STAT3 小分子抑制剂。
J Med Chem. 2013 Jun 13;56(11):4402-12. doi: 10.1021/jm400080c. Epub 2013 May 16.
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Alpha-Based Multiplexed Assay for Identifying SH2 Domain Antagonists.用于鉴定SH2结构域拮抗剂的基于α的多重分析
Methods Mol Biol. 2017;1555:351-356. doi: 10.1007/978-1-4939-6762-9_19.
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Antitumor activity of a novel oral signal transducer and activator of transcription 3 inhibitor YHO-1701.新型口服信号转导子和转录激活子 3 抑制剂 YHO-1701 的抗肿瘤活性。
Cancer Sci. 2020 May;111(5):1774-1784. doi: 10.1111/cas.14369. Epub 2020 Mar 24.
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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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Evaluation of quantitative assays for the identification of direct signal transducer and activator of transcription 3 (STAT3) inhibitors.用于鉴定直接信号转导和转录激活因子3（STAT3）抑制剂的定量分析方法的评估
Oncotarget. 2016 Nov 22;7(47):77998-78008. doi: 10.18632/oncotarget.12868.
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Small Molecule Induces Time-Dependent Inhibition of Stat3 Dimerization and DNA-Binding Activity and Regresses Human Breast Tumor Xenografts.小分子诱导 Stat3 二聚体和 DNA 结合活性的时间依赖性抑制作用，并使人乳腺癌异种移植瘤消退。
Chembiochem. 2024 Nov 18;25(22):e202400351. doi: 10.1002/cbic.202400351. Epub 2024 Oct 23.
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A cell-permeable Stat3 SH2 domain mimetic inhibits Stat3 activation and induces antitumor cell effects in vitro.一种细胞通透型 Stat3 SH2 结构域模拟物可抑制 Stat3 激活并在体外诱导抗肿瘤细胞效应。
J Biol Chem. 2010 Nov 12;285(46):35855-65. doi: 10.1074/jbc.M110.154088. Epub 2010 Aug 31.
引用本文的文献
1
Photoswitchable Stat3 inhibitors: design, synthesis and anticancer activity study on 2D and 3D breast cancer cell cultures.可光开关的信号转导与转录激活因子3（Stat3）抑制剂：二维和三维乳腺癌细胞培养物中的设计、合成及抗癌活性研究
RSC Med Chem. 2025 Jun 6. doi: 10.1039/d5md00490j.
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Identification of insulin-sensitizing molecules acting by disrupting the interaction between the Insulin Receptor and Grb14.鉴定通过破坏胰岛素受体和 Grb14 之间相互作用而起作用的胰岛素增敏分子。
Sci Rep. 2017 Dec 4;7(1):16901. doi: 10.1038/s41598-017-17122-6.
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Identification of novel inhibitors that disrupt STAT3-DNA interaction from a γ-AApeptide OBOC combinatorial library.从一个γ-氨基酸肽基于珠的组合文库中鉴定破坏STAT3与DNA相互作用的新型抑制剂。
Chem Commun (Camb). 2014 Aug 14;50(63):8739-42. doi: 10.1039/c4cc03909b. Epub 2014 Jun 25.
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Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.鉴定氯硝柳胺为信号转导和转录激活因子3（STAT3）信号通路的新型小分子抑制剂
ACS Med Chem Lett. 2010 Sep 7;1(9):454-9. doi: 10.1021/ml100146z. eCollection 2010 Dec 9.
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Structure-Activity Studies of Phosphopeptidomimetic Prodrugs Targeting the Src Homology 2 (SH2) Domain of Signal Transducer and Activator of Transcription 3 (Stat3).靶向信号转导与转录激活因子3（Stat3）的Src同源2（SH2）结构域的磷酸肽模拟前药的构效关系研究
Int J Pept Res Ther. 2013 Mar;19(1):3-12. doi: 10.1007/s10989-012-9313-0.
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Could signal transducer and activator of transcription 3 be a therapeutic target in obesity-related gastrointestinal malignancy?转录信号转导子和激活子3能否成为肥胖相关胃肠道恶性肿瘤的治疗靶点？
J Gastrointest Cancer. 2014 Mar;45(1):1-11. doi: 10.1007/s12029-013-9555-x.
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STAT signaling in the pathogenesis and treatment of myeloid malignancies.信号转导与转录激活因子（STAT）信号通路在髓系恶性肿瘤发病机制及治疗中的作用
JAKSTAT. 2012 Apr 1;1(2):55-64. doi: 10.4161/jkst.20006.
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Targeting STAT3 inhibits growth and enhances radiosensitivity in head and neck squamous cell carcinoma.靶向 STAT3 抑制头颈鳞状细胞癌的生长并增强放射敏感性。
Oral Oncol. 2012 Dec;48(12):1220-6. doi: 10.1016/j.oraloncology.2012.06.006. Epub 2012 Jul 6.
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Structure-based identification and neutralization mechanism of tyrosine sulfate mimetics that inhibit HIV-1 entry.基于结构的鉴定和中和机制的酪氨酸硫酸盐类似物，抑制 HIV-1 进入。
ACS Chem Biol. 2011 Oct 21;6(10):1069-77. doi: 10.1021/cb200068b. Epub 2011 Aug 5.
10
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.
本文引用的文献
1
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.
2
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.
3
Structural basis for the binding of high affinity phosphopeptides to Stat3.高亲和力磷酸肽与Stat3结合的结构基础。
Biopolymers. 2008;90(1):69-79. doi: 10.1002/bip.20901.
4
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.
5
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.
6
Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.通过拟肽探针实现对STAT1或STAT3同二聚化的亚型选择性抑制：STAT SH2结构域的结构识别
Bioorg Med Chem Lett. 2007 Apr 1;17(7):1875-8. doi: 10.1016/j.bmcl.2007.01.077. Epub 2007 Jan 27.
7
Stattic: a small-molecule inhibitor of STAT3 activation and dimerization.Stattic：一种STAT3激活和二聚化的小分子抑制剂。
Chem Biol. 2006 Nov;13(11):1235-42. doi: 10.1016/j.chembiol.2006.09.018.
8
Solid-phase synthesis of Stat3 inhibitors incorporating O-carbamoylserine and O-carbamoylthreonine as glutamine mimics.以O-氨甲酰基丝氨酸和O-氨甲酰基苏氨酸作为谷氨酰胺模拟物的Stat3抑制剂的固相合成。
Bioorg Med Chem Lett. 2007 Feb 1;17(3):654-6. doi: 10.1016/j.bmcl.2006.10.099. Epub 2006 Nov 6.
9
Investigation of the binding determinants of phosphopeptides targeted to the SRC homology 2 domain of the signal transducer and activator of transcription 3. Development of a high-affinity peptide inhibitor.针对信号转导与转录激活因子3的SRC同源2结构域的磷酸肽结合决定簇的研究。一种高亲和力肽抑制剂的开发。
J Med Chem. 2005 Oct 20;48(21):6661-70. doi: 10.1021/jm050513m.
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Validating Stat3 in cancer therapy.验证Stat3在癌症治疗中的作用。
Nat Med. 2005 Jun;11(6):595-6. doi: 10.1038/nm0605-595.
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