进一步功能研究表明,原癌基因酪氨酸蛋白激酶(Src)和含Src同源2结构域蛋白酪氨酸磷酸酶(SHP2)介导FXR Y67位点的磷酸化修饰,FGF-15能够激活成纤维细胞生长因子受体4(FGFR4)-Src级联效应,导致FXR由胞浆向胞核转位,最终增强FXR/RXRα异二聚体与...
FXR的结构有如下特点: (1)具典型的核受体结构, 主要由氨基端(N端)的非配体依赖激活域(ligand-independent activation function 1 domain, AF1)、DNA结合域(DNA-binding domain, DBD)、铰链区(hinge region)及羧基端(C端)的配体结合域(ligand-binding domain, LBD)构成, 其中配体结合域LBD含有配体依赖激活域(lig...
FAS是已知的FXR靶基因, FXR激活后可下调FAS的表达, 以促进脂肪分解过程[44]. 肝脏内的胆汁酸激活FXR后, 通过SHP(在LXR/RXR/LRH-1的协同下)抑制固醇元件结合蛋白-1c(sterol regulatory element-binding protein-1c, SREBP-1c), 降低脂肪酸合酶体系中关键酶的表达, 如乙酰辅酶A羧化酶(acetyl-CoA carboxylase,...
Liver genes enriched in FXR/RXR activation pathway IPA analysis of the top 100 probe-sets from theClare, M. LeeManikhandan, A. V. MudaliarD., R. HaggartC., Roland WolfGino, MieleJ., Keith VassDesmond, J. HighamDaniel, Crowther
17-yl]pentanoic acid; AC-262536, 4-(3-hydroxy-8-aza-bicyclo[3.2.1]octyl)-naphthalene-1-carbonitrile; A/B, amino-terminal domain; AF, activation function; AL-438, 10-methoxy-5-(2-propenyl)-2,5-dihydro-2,2,4-trimethyl-1H-(1)benzopyrano(3,4-f)quinoline; AP, activator protein; AR...
Ⅱ和apoA.V 所活化.有研究表明FXR/RXR 不仅 可以负性调节apo.C11I 的表达(Claudel 等.2003),也 可以上调apo.CII 和apoA.V 的表达.此外,FXR 还 可诱导Angptl3 的表达,从而增加VLDL 的清除. FXR 与脂质代谢调节的密切关系以及其在血 管组织的高表达强烈提示FXR 可能参与了某些疾 病特别是动脉粥样...
Structure-activity relationship of bile acids and bile acid analogs in regard to FXR activation. J Lipid Res. 2004;45:132–8. Article CAS PubMed Google Scholar Pellicciari R, Costantino G, Fiorucci S. Farnesoid X receptor: from structure to potential clinical applications. J Med Chem. ...
Google Share on Facebook FXR AcronymDefinition FXRFixer FXRFarnesoid X-Activated Receptor(diabetes) FXRFlash X-Ray FXRFarnesyl X Receptor(antibodies) FXRWinFax Pro Filename Extension Fax Received FXRHarley-Davidson Super Glide motorcycle model
FXR /RXR异二聚体通过与靶基因中称为 FXR反应 元件( FXR response elem en,t FXRE) 的特定核苷 酸序列结合而调节靶基因的转录 ( 图 2) 。典型的 FXRE是一种被 1个核苷酸分隔的 6 核苷酸反向重 复序列 ( IR 1, AGGTCAnTGACCT ) ; 另外也有一 ...
LY2562175 promotes transcriptional activation of human FXR in a cell-based cotransfection assay with EC50 of 193 nM. S6413 fexaramine Fexaramine is a potent, selective farnesoid X receptor (FXR) agonist with an EC50 of 25 nM and it displays no activity at hRXRα, hPPARα, hPPARγ, h...