Weston Park Cancer Centre and Division of Clinical Medicine, School of Medicine and Population Health, Faculty of Health, University of Sheffield, Sheffield, United Kingdom.
Vancouver Prostate Centre and Department of Experimental Medicine, University of British Columbia, Vancouver, British Columbia, Canada.
Cancer Res. 2024 Jan 2;84(1):9-16. doi: 10.1158/0008-5472.CAN-23-1290.
The one-carbon folate enzyme methylenetetrahydrofolate dehydrogenase/cyclohydrolase 2 (MTHFD2) is a promising therapeutic target in cancer. MTHFD2 is upregulated across numerous cancer types, promotes growth and metastasis of cancer, and correlates with poorer survival. Recent studies have developed small-molecule inhibitors to the isozymes MTHFD2 and MTHFD1 that show promise as anticancer agents through different mechanisms. This review discusses the current understanding of the function of MTHFD2 in cancer and the status of inhibitors for treating MTHFD2-overexpressing cancers.
一碳叶酸酶亚甲基四氢叶酸脱氢酶/环水合酶 2(MTHFD2)是癌症治疗的一个有前途的靶点。MTHFD2 在多种癌症类型中上调,促进癌症的生长和转移,并与较差的生存相关。最近的研究开发了同工酶 MTHFD2 和 MTHFD1 的小分子抑制剂,通过不同的机制显示出作为抗癌剂的潜力。本文讨论了目前对 MTHFD2 在癌症中的作用的理解,以及治疗 MTHFD2 过表达癌症的抑制剂的现状。