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多药耐药相关蛋白的生物学特性与作用机制的研究进展 被引量：11

Adervances in the research of multidrug resistance-associated protein's biological characters and mechanism
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摘要 多药耐药相关蛋白 (MRP1)是ATP结合的盒式 (ABC)膜转运蛋白家族成员 ,基因敲除实验表明MRP1存在与否不影响小鼠正常的生存和各项生理指标 ,生理条件下 ,它可能作为耗能泵将游离的谷胱甘肽和某种尚不了解的内源性代谢物一起泵出细胞外 ,维持细胞外的还原环境。MRP1通过介导细胞内药物排出 ,改变药物在细胞内分布引起肿瘤耐药。 Multidrug-resistance associated protein (MRP), a member of ATP-binding cassette superfamily transporters,confers multi-drug resistance by reducting intracellular drug concentrations and/or altering the pattern of intracellular drug distribution. Using mrp gene knockout models, researchers have found that a total block of mrp is compatible with life and its physiological functions seem to be an ATP-depending pump to co-transport free GSH and some presently unknown endogenous metabolites to protect the normal extracellular environment.
作者 孔肇路
机构地区 复旦大学医学院附属放射医学研究所
出处 《中国癌症杂志》 CAS CSCD 2001年第4期375-378,共4页 China Oncology
关键词 多药耐药相关蛋白 多药耐药性 ABC转运蛋白 肿瘤 MRP1 生物学特性 multidrug-resistance associated protein multidrug resistance ATP-binding cassette superfamily transporters
分类号 R730.21 [医药卫生—肿瘤]
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参考文献14

  • 1[1]Cole SPC, Bhardwai G, Gerlach JH, et al. Overexpression of a novel transporter gene in a multidrug resistant human lung cancer cell line[J]. Science,1992,258(5088):1650-1654.
  • 2[2]Stride BD, Valdimarsson G, Gerlach JH, et al. Structure and expression of the messenger RNA encoding the murine multidrug resistance protein,an ATP-binding cassette transporter[J]. Mol Pharmacol,1996,49(6):962-971.
  • 3[3]Rappa G, Finch RA, Sartrelli AC, et al. New insights into the biology and pharmacology of the multidrug resistance protein(MRP) from gene knockout models[J]. Biochem Pharmacol,1999,58(4):557-562.
  • 4[4]Zaman GJR, Versantvoort CHM, Sdmit JJM,et al. Analysis of the expression of MRP,the gene for a new putative transmembrane drug transporter, in human multidrug resistantcer cell lines[J]. Cancer Res,1993,53(4):1747-1750.
  • 5[5]Zaman GJR, Flens MJ, Vanleusden MR.et al. The human multidrug resistance-associated protein MRP is a plasma membrane drug-efflux pump[J]. Proc Natl Acad Sci USA,1994,91(19):8822-8826.
  • 6[6]Lorico A, Rappa G, Finch RA,et al. Disruption of the murine MRP(multidrug resistance protein) gene leads to increased sensitivity to etoposide (VP-16) and increased levels of glutathione[J]. Cancer Res,1997,57(23):5238-5242.
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  • 8[8]Kuo MT, Bao JJ, Furuichi M, et al.Frequent coexpression of MRP/GS-x pump and γ-glutamylcysteine synthetase mRNA in drug-resistant cells, untreated tumor cells, and normal mouse tissues[J]. Biochem Pharmacol,1998,55(5):605-615.
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中国癌症杂志
2001年 第4期

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