Department of Pathology and Immunology, Washington University School of Medicine, St. Louis, Missouri, United States of America.
Department of Research Biology, Genentech, South San Francisco, California, United States of America.
PLoS One. 2018 Mar 29;13(3):e0194998. doi: 10.1371/journal.pone.0194998. eCollection 2018.
Given the frequency with which MAP kinase signaling is dysregulated in cancer, much effort has been focused on inhibiting RAS signaling for therapeutic benefit. KSR1, a pseudokinase that interacts with RAF, is a potential target; it was originally cloned in screens for suppressors of constitutively active RAS, and its deletion prevents RAS-mediated transformation of mouse embryonic fibroblasts. In this work, we used a genetically engineered mouse model of pancreatic cancer to assess whether KSR1 deletion would influence tumor development in the setting of oncogenic RAS. We found that Ksr1-/- mice on this background had a modest but significant improvement in all-cause morbidity compared to Ksr1+/+ and Ksr1+/- cohorts. Ksr1-/- mice, however, still developed tumors, and precursor pancreatic intraepithelial neoplastic (PanIN) lesions were detected within a similar timeframe compared to Ksr1+/+ mice. No significant differences in pERK expression or in proliferation were noted. RNA sequencing also did not reveal any unique genetic signature in Ksr1-/- tumors. Further studies will be needed to determine whether and in what settings KSR inhibition may be clinically useful.
鉴于 MAP 激酶信号在癌症中经常失调,人们已经投入大量精力来抑制 RAS 信号以获得治疗效果。KSR1 是一种与 RAF 相互作用的拟激酶,是一个潜在的靶点;它最初是在筛选组成性激活 RAS 的抑制剂时被克隆的,其缺失可防止 RAS 介导的小鼠胚胎成纤维细胞转化。在这项工作中,我们使用了一种胰腺癌的基因工程小鼠模型,以评估 KSR1 缺失是否会影响致癌性 RAS 背景下的肿瘤发展。我们发现,与 Ksr1+/+和 Ksr1+/- 队列相比,这种背景下的 Ksr1-/- 小鼠在全因发病率方面有适度但显著的改善。然而,Ksr1-/- 小鼠仍会发生肿瘤,并且与 Ksr1+/+ 小鼠相比,在相似的时间内检测到胰腺上皮内瘤变(PanIN)前病变。ERK 表达或增殖没有明显差异。RNA 测序也没有发现 Ksr1-/- 肿瘤中有任何独特的遗传特征。需要进一步研究以确定 KSR 抑制在何种情况下以及在何种情况下可能具有临床应用价值。