中文摘要：

血管生成对肿瘤的发生、生长和转移至关重要。血管内皮细胞分化、形成新生血管的过程离不开新陈代谢的能量供给和调控作用,尤其是糖酵解途径对肿瘤血管生成的起始点——血管出芽具有非常重要的作用。研究发现,糖酵解过程中的一个关键限速酶——磷酸果糖激酶-2/果糖-2,6-二磷酸酶3（phosphofructokinase-2/fructose-2,6-bisphosphatase 3,PFKFB3）具有较强的激酶活性,若抑制其活性可降低糖酵解速率,从而抑制血管出芽,影响肿瘤血管生成。已经证实,PFKFB3的抑制剂3PO[3-（3-pyridinyl）-1-（4-pyridinyl）-2-propen-1-one]可以显著减少糖酵解,从而抑制病理性血管的生成。因此,近年来通过抑制或破坏肿瘤血管内皮细胞的新陈代谢来进行肿瘤治疗的新方案已成为肿瘤医学领域中一个新的研究热点。本文就内皮细胞糖酵解过程中PFKFB3对肿瘤血管生成的作用,以及以PFKFB3为靶点的肿瘤治疗研究进展进行综述。

英文摘要：

Angiogenesis is essential for the occurrence, growth and metastasis of tumors. The differentiation and neovascularization of vascular endothelial cells depend on the energy supply by metabolism and its regulation, especially the glycolysis pathway is very important for vascular sprouting which is a starting point in the process of tumor angiogenesis. It has been found that phosphofructokinase-2/ fructose-2,6-bisphosphatase 3 （PFKFB3）, a key rate-limiting enzyme of glycolysis pathway, has strong kinase activity. If the activity of PFKFB3 is inhibited, the rate of glycolysis can be reduced, thereby the vascular sprouting in tumor angiogenesis can be blocked. It has been demonstrated that PFKFB3 inhibitor 3-（3-pyridinyl）-1-（4-pyridinyl）- 2-propen-l-one （3PO） can prominently reduce glycolysis and inhibit the pathologic angiogenesis. Therefore, in recent years, it becomes a new research hotspot in the field of cancer therapy to inhibit or destroy the metabolism of tumor vascular endothelial cells for the purpose of curing cancer. This review summarizes the effect of PFKFB3 in glycolysis of endothelial cells on tumor angiogenesis, and the research progress in PFKFB3 as a target for cancer treatment.