Cancer Institute a Key Laboratory for Cancer Prevention & Intervention, National Ministry of Education, The Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, Zhejiang, China.
Cancer Lett. 2012 Mar 28;316(2):204-10. doi: 10.1016/j.canlet.2011.10.039. Epub 2011 Nov 4.
Pyruvate kinase M2 (PKM2) is a rate-limiting enzyme of aerobic glycolysis in cancer cells and plays important roles in cancer metabolism and growth. Here we show that vitamin K(3) and K(5) (VK(3) and VK(5)) are relatively specific PKM2 inhibitors. VK(3) and VK(5) showed a significantly stronger potency to inhibit PKM2 than to inhibit PKM1 and PKL, 2 other isoforms of PK dominantly expressed in most adult tissues and liver. This study combined with previous reports supports that VK(3) and VK(5) have potential as adjuvant for cancer chemotherapy.
丙酮酸激酶 M2 (PKM2) 是癌细胞有氧糖酵解的限速酶，在癌症代谢和生长中发挥重要作用。在这里，我们表明维生素 K(3) 和 K(5) (VK(3) 和 VK(5)) 是相对特异的 PKM2 抑制剂。VK(3) 和 VK(5) 对 PKM2 的抑制作用明显强于对 PKM1 和 PKL 的抑制作用，PKM1 和 PKL 是在大多数成人组织和肝脏中表达的另外两种同工酶。这项研究结合以前的报告表明，VK(3) 和 VK(5) 具有作为癌症化疗辅助剂的潜力。
