Skalnik D G, Brown D A, Brown P C, Friedman R L, Hardeman E C, Schimke R T, Simoni R D
J Biol Chem. 1985 Feb 25;260(4):1991-4.
We have isolated three mammalian cell lines which are resistant to compactin, a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. The drug resistance in all three cell lines is due to an increase of HMG-CoA reductase activity. Two of the three cell lines overaccumulate HMG-CoA reductase messenger RNA when grown in the presence of compactin. DNA hybridization experiments indicate that both a baby hamster kidney-derived compactin-resistant cell line, C100, and a cell line derived from mouse 3T6 cells, 3T6-40, exhibit amplifications of the HMG-CoA reductase gene. A third compactin-resistant cell line derived from Chinese hamster ovary cells, ML100, does not exhibit an amplification of the HMG-CoA reductase gene, nor does it show an elevated level of HMG-CoA reductase mRNA, comparable to that seen in the other cell lines.
我们分离出了三种对洛伐他汀具有抗性的哺乳动物细胞系,洛伐他汀是3-羟基-3-甲基戊二酰辅酶A(HMG-CoA)还原酶的竞争性抑制剂。这三种细胞系中的耐药性均归因于HMG-CoA还原酶活性的增加。当在洛伐他汀存在的情况下生长时,三种细胞系中的两种会过度积累HMG-CoA还原酶信使核糖核酸。DNA杂交实验表明,源自幼仓鼠肾的洛伐他汀抗性细胞系C100和源自小鼠3T6细胞的细胞系3T6-40均表现出HMG-CoA还原酶基因的扩增。源自中国仓鼠卵巢细胞的第三种洛伐他汀抗性细胞系ML100既未表现出HMG-CoA还原酶基因的扩增,也未显示出与其他细胞系中所见水平相当的HMG-CoA还原酶信使核糖核酸水平升高。