Transport Mechanisms and Their Pathology-Induced Regulation Govern Tyrosine Kinase Inhibitor Delivery in Rheumatoid Arthritis
作者: Christian Schmidt-LauberSaliha HarrachThomas PapMeike FischerMarion VictorMarianne HeitzmannUwe HansenManfred FobkerStefan-Martin BrandAleksandra SindicHermann PavenstädtBayram EdemirEberhard SchlatterJessica BertrandGiuliano Ciarimboli
作者单位: 11 Experimental Nephrology, Department of Internal Medicine D, University Hospital Münster, Münster, Germany
2 2 Institute of Experimental Musculoskeletal Medicine, University Hospital Münster, Münster, Germany
3 3 Institute for Physiological Chemistry and Pathobiochemistry, University Hospital Münster, Münster, Germany
4 4 Center of Laboratory Medicine, University Hospital Münster, Münster, Germany
5 5 Leibniz-Institute for Arteriosclerosis Research, University Hospital Münster, Münster, Germany
6 6 Molecular Genetics of Cardiovascular Disease, Institute of Sports Medicine, University Hospital Münster, Münster, Germany
7 7 Department of Physiology, Croatian Institute for Brain Research, University of Zagreb, Zagreb, Croatia
刊名: PLOS ONE, 2012, Vol.7 (12)
来源数据库: PLOS
DOI: 10.1371/journal.pone.0052247
原始语种摘要: Tyrosine kinase inhibitors (TKIs) are effective in treating malignant disorders and were lately suggested to have an impact on non-malignant diseases. However, in some inflammatory conditions like rheumatoid arthritis (RA) the in vivo effect seemed to be moderate. As most TKIs are taken up actively into cells by cell membrane transporters, this study aimed to evaluate the role of such transporters for the accumulation of the TKI Imatinib mesylates in RA synovial fibroblasts as well as their regulation under inflammatory conditions.;;The transport and accumulation of Imatinib was investigated in transporter-transfected HEK293 cells and human RA synovial fibroblasts (hRASF). Transporter expression was quantified by qRT-PCR. In transfection experiments, hMATE1 showed the highest apparent...
全文获取路径: PLOS 
影响因子:3.73 (2012)

  • transport 输运
  • Tyrosine 酪氨酸
  • expression 表示
  • knockdown 击倒
  • transfection 转染
  • conditions 条件式
  • indeed 的确
  • evaluate 求...的值
  • synovial 关节的
  • cytokines 细胞浆移动