ABCB1 pharmacogenetics:: Progress, pitfalls, and promise
ABCB1 pharmacogenetics:: Progress, pitfalls, and promise
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DOI：
10.1038/sj.clpt.6100052
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发表时间：
2007-02-01
影响因子：
6.7
通讯作者：
Kroetz, D. L.
中科院分区：
文献类型：
--
作者：
Chinn, L. W.;Kroetz, D. L.
1976年，Juliano和Ling（1）报道了一种170 kDa的蛋白质在秋水仙素抗性中国仓鼠卵巢（CHO）细胞中的表达，而这种蛋白质在药物敏感细胞中是不存在的。由于这种蛋白质改变了细胞对秋水仙碱的渗透性，作者将其命名为P-糖蛋白（P-gp）。(1)P-gp过度表达在肿瘤样本和白血病细胞中被描述。2与细菌转运蛋白的高度同源性表明P-gp是一种外排转运蛋白，调节细胞内外源性物质的浓度。1986年，发现了编码P-gp的基因并命名为MDR 1（HUGO名称ABCB 1）。(4)免疫组化研究表明，P-gp表达在组织分泌或排泄功能（肝，肾，胃肠道）和血液-4问题的屏障网站，如血脑屏障。(5)这种表达模式表明P-gp可能通过药代动力学或药效学效应影响异生素反应和毒性。（六）
In 1976, Juliano and Ling(1) reported expression of a 170 kDa protein in colchicine-resistant Chinese hamster ovary (CHO) cells that was absent in drug-sensitive cells. Because this protein altered cellular permeability to colchicine, the authors named it P-glycoprotein (P-gp).(1) P-gp overexpression was described in tumor samples and leukemic cells. 2 High homology with bacterial transporters suggested that P-gp was an efflux transporter, modulating intracellular xenobiotic concentrations. In 1986, the gene encoding P-gp was discovered and designated MDR1 (HUGO name ABCB1).(4) Immunohistochemical studies demonstrated P-gp expression in tissues with secretory or excretory functions (liver, kidney, and gastrointestinal tract) and at blood-4issue barrier sites, such as the blood-brain barrier.(5) This pattern of expression indicated that P-gp may influence xenobiotic response and toxicity, either through pharmacokinetic or pharmacodynamic effects.(6)