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小分子抑制剂LDYS-14007对JAK1-STAT3信号通路的影响研究

Study on the effect of small molecule inhibitors LDYS-14007 on JAK1-STAT3 signaling pathway
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摘要 目的:研究LDYS-14007对JAK1-STAT3信号通路的影响。方法分别用10μmol 、1 nmol 的LDYS-14007和10μmol的Tofacitinib处理MDA-MB-231细胞。用Western blot法检测JAK1和STAT3的蛋白表达以及磷酸化状况。结果吸光度A与蛋白质浓度C呈线性相关,线性方程为A=0.0075C+0.0029,r=0.9976,线性范围为1.08~5.08 mg/mL;随着LDYS-14007浓度的增加, Phospho-JAK1,Phospho-STAT3的量逐渐减少。结论 LDYS-14007可通过降低JAK1和STAT3的磷酸化水平抑制JAK1-STAT3信号通路。 LDYS-14007可能在类风湿性关节炎( rheumatoid arthritis, RA)的治疗中起重要作用。 Objective To study the effect of LDYS-14007 on JAK1-STAT3 signaling pathways.Methods MDA-MB-231 cells were treated with 10μmol,1 nmol LDYS-14007, and 10 μmol Tofacitinib,respectively.Western blot assay was used to determine the expression of JAK1,Phospho-JAK1, STAT3 and Phospho-STAT3.Results The absorbance value was linearly related to the concentration of protein C, The linear equation is A=0.0075C+0.0029, r=0.9976, The linear range of 1.08-5.08 mg/mL, With the increased concentration of LDYS-14007, the amount of Phospho-JAK1, Phospho-STAT3 were all gradually decreased.Conclusion LDYS-14007 leads to the levels of Phospho-JAK1 and Phospho-STAT3 decrease, which inhibits JAK1-STAT3 signaling pathway.LDYS-14007 may play an important role in the treatment of rheumatoid arthritis.
机构地区 聊城大学药学院
出处 《中国生化药物杂志》 CAS 2015年第6期10-12,共3页 Chinese Journal of Biochemical Pharmaceutics
基金 国家高新技术研究发展计划(863计划 2012AA02A306)
关键词 LDYS-14007 JAK-STAT信号通路 类风湿性关节炎 LDYS-14007 JAK1-STAT3 signaling pathways rheumatoid arthritis
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参考文献10

  • 1Stark GR, Damell JE Jr. The JAK-STAT pathway at twenty [ J ]. Immunity,2012, 36(4) : 503-514.
  • 2Kontzias A,Kotlyar A, Laurence A, et al. Jakinibs: a new class of kinase inhibitors in cancer and autoimmune disease [ J ]. Curt Opin Pharmacol,2012,12(4) : 464-470.
  • 3Laurence A, Pesu M, Silvennoinen O, et al. JAK Kinases in Health and Disease: An Update[ J]. Open Rheumatol J,2012,6: 232-244.
  • 4Scott DL, Wolfe F, Huizinga TW. Rheumatoid arthritis [ J ]. Lancet, 2010,376(9746) : 1094-1108.
  • 5Smolen JS, Aletaha D, Bijlsma JW, et al. Treating rheumatoid arthritis to target: recommendations of an international task force [ J ]. Ann Rheumatic Dis, 2010,69(4) : 631-637.
  • 6Moran N. Incyte comes of age with JAK inhibitor approval [ J ]. Nat Biotechnal, 2012,30(1): 3-5.
  • 7刘文哲,李金瀚,胡义德,钱桂生.顺铂诱导A549细胞凋亡的研究[J].中国肺癌杂志,2002,5(4):254-256. 被引量:13
  • 8Hollan I, Dessein PH, Ronda N, et al. Prevention of cardiovascular disease in rheumatoid arthritis [ J ]. Autoimmun Rev, 2015. DOI: 1~3. 1016/j. 06. 004. antrev. 2015.
  • 9Smolen JS, Landewe R, Breedveld FC, et al. EULAR recommendations for the management of rheumatoid arthritis with synthetic and biological disease-modifying antirheumatic drugs: 2013 update [ J~. Ann Rheum Dis, 2014,73(3) : 492-509.
  • 10Migita K,Izumi ~, Torigoshi T, et al. Inhibition of Janus kinase/signal transducer and activator of transcription (JAK/STAT) signalling pathway in rheumatoid synovial fibroblasts using small molecule compounds [ J 1. Clin Exp Immunol, 2013,174 ( 3 ) : 356-363.

二级参考文献5

  • 1[3]Fan W,Everett ET,Tan C,et al.Glucocorticoid-mediated inhibition of toxol-induced apoptosis in leiomyosarcoma cells.Cell Pharmacol,1994,1(2)∶205-213.
  • 2[4]Miquel K,Pradines A,Favre G.Farnesol and geranylgeraniol induce actin cytoskeleton disorganization and apoptosis in A549 lung adenocarcinoma cells.Biochem Biophys Res Commun,1996,225(3)∶869-876.
  • 3[5]Efferth T,Rucker G,Falkenberg M,et al.Detection of apoptosis in KG-1α Leukemic cells treated with investigational drugs.Arzneimittel Forschung,1996,46(2)∶196-200.
  • 4[1]Lowe SW,Ruley HE,Jacks T,et al.p53-dependent apoptosis modulates the cytotoxicity of anticancer agents.Cell,1993,74(6)∶957-967.
  • 5[2]Lutzker SG,Levine AJ.Apoptosis and cancer chemotherapy.Cancer Treat Res,1996,87∶345-356.

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