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Identification of small molecule inhibitors of p27(Kip1) ubiquitination by high-throughput screening.通过高通量筛选鉴定 p27(Kip1)泛素化的小分子抑制剂。
Cancer Sci. 2013 Nov;104(11):1461-7. doi: 10.1111/cas.12246. Epub 2013 Sep 6.
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High-throughput screening AlphaScreen assay for identification of small-molecule inhibitors of ubiquitin E3 ligase SCFSkp2-Cks1.用于鉴定泛素E3连接酶SCFSkp2-Cks1小分子抑制剂的高通量筛选AlphaScreen检测法
J Biomol Screen. 2013 Sep;18(8):910-20. doi: 10.1177/1087057113485789. Epub 2013 Apr 15.
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Specific small molecule inhibitors of Skp2-mediated p27 degradation.Skp2介导的p27降解的特异性小分子抑制剂。
Chem Biol. 2012 Dec 21;19(12):1515-24. doi: 10.1016/j.chembiol.2012.09.015.
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Inhibitors of SCF-Skp2/Cks1 E3 ligase block estrogen-induced growth stimulation and degradation of nuclear p27kip1: therapeutic potential for endometrial cancer.SCF-Skp2/Cks1 E3 连接酶抑制剂阻断雌激素诱导的生长刺激和核 p27kip1 的降解：子宫内膜癌的治疗潜力。
Endocrinology. 2013 Nov;154(11):4030-45. doi: 10.1210/en.2013-1757. Epub 2013 Sep 13.
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Structural basis of the Cks1-dependent recognition of p27(Kip1) by the SCF(Skp2) ubiquitin ligase.SCF（Skp2）泛素连接酶依赖Cks1识别p27（Kip1）的结构基础。
Mol Cell. 2005 Oct 7;20(1):9-19. doi: 10.1016/j.molcel.2005.09.003.
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Mutant B-RAF signaling and cyclin D1 regulate Cks1/S-phase kinase-associated protein 2-mediated degradation of p27Kip1 in human melanoma cells.突变型B-RAF信号传导和细胞周期蛋白D1调节人黑素瘤细胞中Cks1/细胞周期蛋白依赖性激酶调节亚基1介导的p27Kip1降解。
Oncogene. 2007 Feb 15;26(7):1056-66. doi: 10.1038/sj.onc.1209861. Epub 2006 Aug 21.
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Cks1 promotion of S phase entry and proliferation is independent of p27Kip1 suppression.Cks1 促进 S 期进入和增殖与抑制 p27Kip1 无关。
Mol Cell Biol. 2012 Jul;32(13):2416-27. doi: 10.1128/MCB.06771-11. Epub 2012 Apr 16.
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PTEN regulates the ubiquitin-dependent degradation of the CDK inhibitor p27(KIP1) through the ubiquitin E3 ligase SCF(SKP2).PTEN通过泛素E3连接酶SCF（SKP2）调节细胞周期蛋白依赖性激酶抑制剂p27（KIP1）的泛素依赖性降解。
Curr Biol. 2001 Feb 20;11(4):263-7. doi: 10.1016/s0960-9822(01)00065-3.
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Inhibition of F-Box protein p45(SKP2) expression and stabilization of cyclin-dependent kinase inhibitor p27(KIP1) in vitamin D analog-treated cancer cells.维生素D类似物处理的癌细胞中F-Box蛋白p45（SKP2）表达的抑制及细胞周期蛋白依赖性激酶抑制剂p27（KIP1）的稳定化
Endocrinology. 2003 Mar;144(3):749-53. doi: 10.1210/en.2002-0026.
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Degradation of p27(Kip1) at the G(0)-G(1) transition mediated by a Skp2-independent ubiquitination pathway.在由独立于Skp2的泛素化途径介导的G(0)-G(1)转变过程中p27(Kip1)的降解
J Biol Chem. 2001 Dec 28;276(52):48937-43. doi: 10.1074/jbc.M107274200. Epub 2001 Oct 26.
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SKping cell cycle regulation: role of ubiquitin ligase SKP2 in hematological malignancies.跳过细胞周期调控：泛素连接酶SKP2在血液系统恶性肿瘤中的作用
Front Oncol. 2024 Mar 15;14:1288501. doi: 10.3389/fonc.2024.1288501. eCollection 2024.
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Thioridazine reverses trastuzumab resistance in gastric cancer by inhibiting S-phase kinase associated protein 2-mediated aerobic glycolysis.噻吨嗪通过抑制 S 期激酶相关蛋白 2 介导的有氧糖酵解逆转胃癌中的曲妥珠单抗耐药性。
World J Gastroenterol. 2023 Dec 7;29(45):5974-5987. doi: 10.3748/wjg.v29.i45.5974.
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Small-molecule compounds inhibiting S-phase kinase-associated protein 2: A review.抑制S期激酶相关蛋白2的小分子化合物综述
Front Pharmacol. 2023 Apr 5;14:1122008. doi: 10.3389/fphar.2023.1122008. eCollection 2023.
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Potential Therapeutics Targeting Upstream Regulators and Interactors of EHMT1/2.针对EHMT1/2上游调节因子和相互作用分子的潜在治疗方法。
Cancers (Basel). 2022 Jun 9;14(12):2855. doi: 10.3390/cancers14122855.
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Phytochemical library screening reveals betulinic acid as a novel Skp2-SCF E3 ligase inhibitor in non-small cell lung cancer.植物化学文库筛选发现白桦脂酸可抑制非小细胞肺癌中的 Skp2-SCF E3 连接酶。
Cancer Sci. 2021 Aug;112(8):3218-3232. doi: 10.1111/cas.15005. Epub 2021 Jun 28.
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Emerging Roles of SKP2 in Cancer Drug Resistance.SKP2 在癌症耐药性中的新兴作用。
Cells. 2021 May 10;10(5):1147. doi: 10.3390/cells10051147.
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Chlorinated Guaiane-Type Sesquiterpene Lactones as Cytotoxic Agents against Human Tumor Cells.氯化愈创木烷型倍半萜内酯作为抗人肿瘤细胞的细胞毒剂
Int J Mol Sci. 2020 Dec 21;21(24):9767. doi: 10.3390/ijms21249767.
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F-Box Proteins and Cancer.F盒蛋白与癌症
Cancers (Basel). 2020 May 15;12(5):1249. doi: 10.3390/cancers12051249.
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The Skp2 Pathway: A Critical Target for Cancer Therapy.Skp2 通路：癌症治疗的关键靶点。
Semin Cancer Biol. 2020 Dec;67(Pt 2):16-33. doi: 10.1016/j.semcancer.2020.01.013. Epub 2020 Feb 1.
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Chemical probes of Skp2-mediated p27 ubiquitylation and degradation.Skp2介导的p27泛素化和降解的化学探针
Medchemcomm. 2018 Jun 11;9(7):1093-1104. doi: 10.1039/c8md00140e. eCollection 2018 Jul 1.
本文引用的文献
1
Chemical genetics approach to restoring p27Kip1 reveals novel compounds with antiproliferative activity in prostate cancer cells.化学遗传学方法恢复 p27Kip1 揭示了具有前列腺癌细胞抗增殖活性的新型化合物。
BMC Biol. 2010 Dec 23;8:153. doi: 10.1186/1741-7007-8-153.
2
Deficiency in chromosome congression by the inhibition of Plk1 polo box domain-dependent recognition.通过抑制Plk1 polo盒结构域依赖性识别导致染色体排列缺陷。
J Biol Chem. 2009 Jan 23;284(4):2344-53. doi: 10.1074/jbc.M805308200. Epub 2008 Nov 25.
3
The Cdk inhibitor p27 in human cancer: prognostic potential and relevance to anticancer therapy.人类癌症中的细胞周期蛋白依赖性激酶抑制剂p27：预后潜力及与抗癌治疗的相关性
Nat Rev Cancer. 2008 Apr;8(4):253-67. doi: 10.1038/nrc2347.
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Targeting the p27 E3 ligase SCF(Skp2) results in p27- and Skp2-mediated cell-cycle arrest and activation of autophagy.靶向p27 E3连接酶SCF（Skp2）会导致p27和Skp2介导的细胞周期停滞以及自噬激活。
Blood. 2008 May 1;111(9):4690-9. doi: 10.1182/blood-2007-09-112904. Epub 2008 Feb 27.
5
Oncogenic properties and prognostic implications of the ubiquitin ligase Skp2 in cancer.泛素连接酶Skp2在癌症中的致癌特性及预后意义
Cancer. 2008 Apr 1;112(7):1415-24. doi: 10.1002/cncr.23317.
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p21 and p27 induction by silibinin is essential for its cell cycle arrest effect in prostate carcinoma cells.水飞蓟宾诱导p21和p27对其在前列腺癌细胞中的细胞周期阻滞作用至关重要。
Mol Cancer Ther. 2007 Oct;6(10):2696-707. doi: 10.1158/1535-7163.MCT-07-0104.
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Structural basis of the Cks1-dependent recognition of p27(Kip1) by the SCF(Skp2) ubiquitin ligase.SCF（Skp2）泛素连接酶依赖Cks1识别p27（Kip1）的结构基础。
Mol Cell. 2005 Oct 7;20(1):9-19. doi: 10.1016/j.molcel.2005.09.003.
8
Small interfering RNA targeting of S phase kinase-interacting protein 2 inhibits cell growth of oral cancer cells by inhibiting p27 degradation.靶向S期激酶相关蛋白2的小分子干扰RNA通过抑制p27降解来抑制口腔癌细胞的生长。
Mol Cancer Ther. 2005 Mar;4(3):471-6. doi: 10.1158/1535-7163.MCT-04-0232.
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Gene therapy for human small-cell lung carcinoma by inactivation of Skp-2 with virally mediated RNA interference.通过病毒介导的RNA干扰使Skp-2失活对人小细胞肺癌进行基因治疗。
Gene Ther. 2005 Jan;12(1):95-100. doi: 10.1038/sj.gt.3302391.
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Skp2-mediated degradation of p27 regulates progression into mitosis.Skp2介导的p27降解调控有丝分裂进程。
Dev Cell. 2004 May;6(5):661-72. doi: 10.1016/s1534-5807(04)00131-5.
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