Ferguson Robert, Aughton Karen, Evans Anthony, Shaw Victoria, Armstrong Jane, Ware Adam, Bennett Laura, Costello Eithne, Greenhalf William
Liverpool Experimental Cancer Medicine Centre, University of Liverpool, Liverpool L3 5TR, UK.
Curr Issues Mol Biol. 2023 Mar 17;45(3):2505-2520. doi: 10.3390/cimb45030164.
The development of K-Ras independence may explain the failure of targeted therapy for pancreatic cancer (PC). In this paper, active N as well as K-Ras was shown in all human cell lines tested. In a cell line dependent on mutant K-Ras, it was shown that depleting K-Ras reduced total Ras activity, while cell lines described as independent had no significant decline in total Ras activity. The knockdown of N-Ras showed it had an important role in controlling the relative level of oxidative metabolism, but only K-Ras depletion caused a decrease in G2 cyclins. Proteasome inhibition reversed this, and other targets of APC/c were also decreased by K-Ras depletion. K-Ras depletion did not cause an increase in ubiquitinated G2 cyclins but instead caused exit from the G2 phase to slow relative to completion of the S-phase, suggesting that the mutant K-Ras may inhibit APC/c prior to anaphase and stabilise G2 cyclins independently of this. We propose that, during tumorigenesis, cancer cells expressing wild-type N-Ras protein are selected because the protein protects cancer cells from the deleterious effects of the cell cycle-independent induction of cyclins by mutant K-Ras. Mutation independence results when N-Ras activity becomes adequate to drive cell division, even in cells where K-Ras is inhibited.
K-Ras非依赖性的发展可能解释了胰腺癌(PC)靶向治疗失败的原因。在本文中,在所有测试的人类细胞系中均显示有活性的N以及K-Ras。在一个依赖突变型K-Ras的细胞系中,研究表明敲低K-Ras会降低总Ras活性,而那些被描述为非依赖性的细胞系总Ras活性则无显著下降。敲低N-Ras显示其在控制氧化代谢的相对水平方面具有重要作用,但只有敲低K-Ras会导致G2期细胞周期蛋白减少。蛋白酶体抑制可逆转这一现象,并且APC/c的其他靶点也会因K-Ras敲低而减少。K-Ras敲低并未导致泛素化的G2期细胞周期蛋白增加,反而相对于S期完成而言,导致从G2期退出的速度减慢,这表明突变型K-Ras可能在后期之前抑制APC/c,并独立于此稳定G2期细胞周期蛋白。我们提出,在肿瘤发生过程中,表达野生型N-Ras蛋白的癌细胞被选择,因为该蛋白可保护癌细胞免受突变型K-Ras非细胞周期依赖性诱导细胞周期蛋白所产生的有害影响。当N-Ras活性足以驱动细胞分裂时,即使在K-Ras被抑制的细胞中,也会产生突变非依赖性。