Zieg J, Clayton C E, Ardeshir F, Giulotto E, Swyryd E A, Stark G R
Mol Cell Biol. 1983 Nov;3(11):2089-98. doi: 10.1128/mcb.3.11.2089-2098.1983.
Eleven independent lines of Syrian hamster cells were selected by using very low levels of N-(phosphonacetyl)-L-aspartate (PALA), an inhibitor of aspartate transcarbamylase. The protocol employed insured that each resistant cell arose during one of the last divisions before selection was applied. Cells of each mutant line contained an amplification of the structural gene for CAD, a trifunctional protein which includes aspartate transcarbamylase and two other enzymes of UMP biosynthesis. Strikingly, despite the minimal selection employed, the degree of amplification of the CAD gene was 6 to 10 times the normal diploid number in all 11 cases. In situ hybridization indicated that the amplified CAD genes were almost always present at a single chromosomal site in each line. Therefore, one of the two alleles was amplified 11- to 19-fold. The rates at which cells became resistant to PALA, determined by fluctuation analysis, were 100 times less dependent on drug concentration than were the frequencies of resistant cells in steady-state populations. The relatively shallow dependence of this rate upon PALA concentration is consistent with our independent observation that most events gave rise to a similar degree of amplification. In six of six cell lines examined, the levels of CAD mRNA and aspartate transcarbamylase activity were elevated two- to fourfold. These lines were resistant to PALA concentrations 20- to 80-fold higher than the ones used for selection. The organization of amplified DNA was examined by hybridizing Southern blots with cloned DNA fragments containing amplified sequences, previously isolated from two cell lines resistant to high levels of PALA. A contiguous region of DNA approximately 44 kilobases long which included the CAD gene was amplified in five of five single-step mutants examined. Outside this region, these mutants shared amplified sequences with only one of the two highly resistant lines.
通过使用极低水平的N-(膦酰乙酰基)-L-天冬氨酸(PALA,天冬氨酸转氨甲酰酶的一种抑制剂),选择出了11个独立的叙利亚仓鼠细胞系。所采用的实验方案确保每个抗性细胞都产生于施加选择之前的最后几次分裂之一。每个突变细胞系的细胞都包含CAD结构基因的扩增,CAD是一种三功能蛋白,其中包括天冬氨酸转氨甲酰酶和UMP生物合成的其他两种酶。引人注目的是,尽管采用的选择压力极小,但在所有11个案例中,CAD基因的扩增程度是正常二倍体数的6至10倍。原位杂交表明,每个细胞系中扩增的CAD基因几乎总是位于单个染色体位点。因此,两个等位基因中的一个被扩增了11至19倍。通过波动分析确定细胞对PALA产生抗性的速率,其对药物浓度的依赖性比稳态群体中抗性细胞的频率低100倍。该速率对PALA浓度的相对较弱依赖性与我们独立观察到的大多数事件导致相似程度的扩增一致。在所检测的六个细胞系中的六个中,CAD mRNA水平和天冬氨酸转氨甲酰酶活性提高了2至4倍。这些细胞系对PALA浓度的抗性比用于选择的浓度高20至80倍。通过将Southern印迹与含有扩增序列的克隆DNA片段杂交来检查扩增DNA的组织,这些片段先前是从两个对高水平PALA有抗性的细胞系中分离出来的。在五个单步突变体中,一个大约44千碱基长的包含CAD基因的连续DNA区域被扩增。在该区域之外,这些突变体仅与两个高抗性细胞系之一共享扩增序列。