Blood Research Institute, Versiti, 8727 Watertown Plank Rd., Milwaukee, WI 53226, USA.
Blood Research Institute, Versiti, 8727 Watertown Plank Rd., Milwaukee, WI 53226, USA; Departments of Cell Biology, Neurobiology, and Anatomy, and Pediatrics, Medical College of Wisconsin, 8701 Watertown Plank Rd., Milwaukee, WI 53226, USA.
Neoplasia. 2020 Nov;22(11):644-658. doi: 10.1016/j.neo.2020.07.001.
Fbw7 is a tumor suppressor that regulates the degradation of oncogenic substrates such as c-Jun, c-Myc, Notch1 intracellular domain (ICD), and cyclin E by functioning as the substrate recognition protein in the Skp1-Cullin-F-box (SCF) ubiquitin ligase complex. Consequently, low expression or loss of FBXW7 in breast cancer has been hypothesized to result in the accumulation of oncogenic transcription factors that are master regulators of proliferation, apoptosis, and ultimately transformation. Despite this, the direct effect of Fbw7 loss on mammary gland morphology and tumorigenesis has not been examined. Here, we demonstrate that conditional deletion of Fbxw7 in murine mammary tissue initiates breast tumor development and also results in lactation and involution defects. Further, while Fbxw7 loss results in the overexpression of Notch1-ICD, c-Jun, cyclin E, and c-Myc, the downstream transcription factor pathways associated with c-Myc and cyclin E are the most dysregulated, including at the single-cell level. These pathways are dysregulated early after Fbxw7 loss, and their sustained loss results in tumorigenesis and reinforced c-Myc and cyclin E-E2F pathway disruption. We also find that loss of Fbxw7 is linked to the acquisition of Trp53 mutations, similar to the mutational spectrum observed in patients. Our results demonstrate that the loss of Fbxw7 promotes the acquisition of Trp53 mutations and that the two cooperate in breast tumor development. Targeting c-Myc, E2F, or p53 may therefore be a beneficial treatment strategy for FBXW7-altered breast cancer patients.
FBXW7 是一种肿瘤抑制因子,通过作为 Skp1-Cullin-F-box(SCF)泛素连接酶复合物中的底物识别蛋白,调节致癌底物(如 c-Jun、c-Myc、Notch1 细胞内结构域(ICD)和细胞周期蛋白 E)的降解。因此,乳腺癌中 FBXW7 的低表达或缺失被假设会导致致癌转录因子的积累,这些转录因子是增殖、凋亡和最终转化的主要调节因子。尽管如此,FBXW7 缺失对乳腺形态和肿瘤发生的直接影响尚未得到检验。在这里,我们证明了 FBXW7 在小鼠乳腺组织中的条件缺失会引发乳腺肿瘤的发生,并且还会导致泌乳和退化缺陷。此外,尽管 FBXW7 的缺失导致 Notch1-ICD、c-Jun、细胞周期蛋白 E 和 c-Myc 的过表达,但与 c-Myc 和细胞周期蛋白 E 相关的下游转录因子途径是最失调的,包括在单细胞水平。这些途径在 FBXW7 缺失后早期失调,其持续缺失会导致肿瘤发生和增强 c-Myc 和细胞周期蛋白 E-E2F 途径的破坏。我们还发现 FBXW7 的缺失与 Trp53 突变的获得有关,类似于在患者中观察到的突变谱。我们的结果表明,FBXW7 的缺失促进了 Trp53 突变的获得,并且两者在乳腺肿瘤的发展中合作。因此,针对 c-Myc、E2F 或 p53 可能是 FBXW7 改变的乳腺癌患者的有益治疗策略。