生物活性

• 靶点	prolyl-tRNA Synthetase Ki:18.3nM

• 描述Halofuginone is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/mL in mammal.
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01978366	Duchenne Muscular Dystrophy	Phase 2	Terminated(Dosing stopped)	-	United States, California ... more >> University of California, Davis Medical Center Sacramento, California, United States, 95817 United States, Maryland Kennedy Krieger Institute, Johns Hopkins School of Medicine Baltimore, Maryland, United States, 21205 United States, Missouri Washington University School of Medicine Saint Louis, Missouri, United States, 63110 United States, Ohio Cincinnati Children's Hospital Medical Center Cincinnati, Ohio, United States, 45229 Nationwide Children's Hospital Columbus, Ohio, United States, 43205 Collapse <<
  NCT01847573	Duchenne Muscular Dystrophy	Phase 1 Phase 2	Terminated(Dosing stopped)	-	United States, California ... more >> University of California, Davis Medical Center Sacramento, California, United States, 95817 United States, Maryland Kennedy Krieger Institute, Johns Hopkins School of Medicine Baltimore, Maryland, United States, 21205 United States, Missouri Washington University School of Medicine Saint Louis, Missouri, United States, 63110 United States, Ohio Cincinnati Children's Hospital Medical Center Cincinnati, Ohio, United States, 45229 Nationwide Children's Hospital Columbus, Ohio, United States, 43205 Collapse <<
  NCT02525302	Duchenne Muscular Dystrophy	Phase 2	Terminated(Dosing stopped)	-	United States, California ... more >> University of California, Davis Medical Center Sacramento, California, United States, 95817 United States, Maryland Kennedy Krieger Institute, Johns Hopkins School of Medicine Baltimore, Maryland, United States, 21205 United States, Missouri Washington University School of Medicine Saint Louis, Missouri, United States, 63110 United States, Ohio Cincinnati Children's Hospital Medical Center Cincinnati, Ohio, United States, 45229 Nationwide Children's Hospital Columbus, Ohio, United States, 43205 Collapse <<

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• 参考文献

• [1] Nelson EF, Huang CW, et al. Halofuginone down-regulates Smad3 expression and inhibits the TGFbeta-induced expression of fibrotic markers in human corneal fibroblasts. Mol Vis. 2012;18:479-87.

  [2] Keller TL, Zocco D, et al. Halofuginone and other febrifugine derivatives inhibit prolyl-tRNA synthetase. Nat Chem Biol. 2012 Feb 12;8(3):311-7.