Department of Systems Biology, Beckman Research Institute, and City of Hope Comprehensive Cancer Center, Monrovia, CA 91016, USA.
Department of Systems Biology, Beckman Research Institute, and City of Hope Comprehensive Cancer Center, Monrovia, CA 91016, USA.
Cell. 2018 Apr 5;173(2):470-484.e18. doi: 10.1016/j.cell.2018.02.048. Epub 2018 Mar 15.
B cell activation during normal immune responses and oncogenic transformation impose increased metabolic demands on B cells and their ability to retain redox homeostasis. While the serine/threonine-protein phosphatase 2A (PP2A) was identified as a tumor suppressor in multiple types of cancer, our genetic studies revealed an essential role of PP2A in B cell tumors. Thereby, PP2A redirects glucose carbon utilization from glycolysis to the pentose phosphate pathway (PPP) to salvage oxidative stress. This unique vulnerability reflects constitutively low PPP activity in B cells and transcriptional repression of G6PD and other key PPP enzymes by the B cell transcription factors PAX5 and IKZF1. Reflecting B-cell-specific transcriptional PPP-repression, glucose carbon utilization in B cells is heavily skewed in favor of glycolysis resulting in lack of PPP-dependent antioxidant protection. These findings reveal a gatekeeper function of the PPP in a broad range of B cell malignancies that can be efficiently targeted by small molecule inhibition of PP2A and G6PD.
B 细胞在正常免疫反应和致癌转化过程中的激活会增加 B 细胞的代谢需求及其维持氧化还原平衡的能力。丝氨酸/苏氨酸蛋白磷酸酶 2A(PP2A)已被确定为多种类型癌症的肿瘤抑制因子,而我们的遗传研究揭示了 PP2A 在 B 细胞肿瘤中的重要作用。因此,PP2A 将葡萄糖碳利用从糖酵解重新定向到磷酸戊糖途径(PPP)以挽救氧化应激。这种独特的脆弱性反映了 B 细胞中 PPP 活性持续降低,以及 B 细胞转录因子 PAX5 和 IKZF1 对 G6PD 和其他关键 PPP 酶的转录抑制。反映 B 细胞特异性转录 PPP 抑制,B 细胞中的葡萄糖碳利用严重偏向糖酵解,导致缺乏 PPP 依赖性抗氧化保护。这些发现揭示了 PPP 在广泛的 B 细胞恶性肿瘤中的守门员功能,可通过小分子抑制 PP2A 和 G6PD 来有效靶向该功能。