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磷酸甘油酸变位酶1及其抑制剂的研究进展

Progress in Research on Phosphoglycerate Mutase 1 and Its Inhibitors

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【作者】 梁倩陈红专沈瑛

【Author】 LIANG Qian;CHEN Hongzhuan;SHEN Ying;Department of Pharmacology and Chemical Biology, School of Medicine, Shanghai Jiao Tong University;Shanghai Collaborative Innovation Center for Translational Medicine;Shanghai University of Traditional Chinese Medicine;

【通讯作者】 沈瑛;

【机构】 上海交通大学医学院药理学与化学生物学系上海市转化医学协同创新中心上海中医药大学

【摘要】 糖酵解通路关键代谢酶磷酸甘油酸变位酶1(PGAM1)催化3-磷酸甘油酸(3-PG)转化为2-磷酸甘油酸(2-PG),参与生物大分子合成和维持细胞内氧化还原稳态,同时具有非酶依赖的蛋白-蛋白相互作用功能,促进肿瘤生长和转移。研究发现,PGAM1在多种恶性肿瘤中普遍高表达且与患者的不良预后密切相关,在肿瘤的发生发展中起着至关重要的作用。PGAM1作为极具潜力的抗肿瘤新靶标,其抑制剂的研发也受到越来越多的关注。综述PGAM1在肿瘤中的作用以及PGAM1抑制剂的最新研究进展。

【Abstract】 As the key metabolic enzyme in the glycolytic pathway, phosphoglycerate mutase 1(PGAM1) participated in the synthesis of intracellular biological macromolecules and maintained redox homeostasis by catalyzing the conversion of 3-phosphoglycerate(3-PG) to 2-phosphoglycerate(2-PG). Increasing evidence has suggested that PGAM1 also conveys metabolism-independent function of protein-protein interaction to aggravate tumor growth and metastasis. PGAM1, which is generally over-expressed in a variety of malignancies and is closely related to the patient’s poor prognosis, plays a vital role in tumor progression. As a novel potential antitumor target, PGAM1 together with the research and development of its inhibitors has attracted great attention. This article reviews the role of PGAM1 in tumors and recent advances in the research on PGAM1 inhibitors.

【基金】 国家自然科学基金面上项目(No.81773748);上海市高水平地方高校建设“药理学创新先导项目”(No.XD18011)
  • 【文献出处】 药学进展 ,Progress in Pharmaceutical Sciences , 编辑部邮箱 ,2020年08期
  • 【分类号】R979.1;R730.2
  • 【下载频次】190
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