鞘氨醇激酶的相关抑制剂研究进展

Progress on the research of sphingosine kinase related inhibitors

鞘氨醇激酶(SphK)是脂质激酶,其作为癌症生物学中的重要限速酶受到了广泛的关注.它们通过产生鞘氨醇-1-磷酸(S1P)参与多种信号通路的调节,而S1P可介导细胞生长、分化、迁移和血管生成等多种生物学功能.目前鞘氨醇激酶抑制剂的研究是国内外研究的热点,并且随着鞘氨醇激酶1(SphK1)晶体结构的解析,更多高选择性、高活性的抑制剂被开发出来.本文综述了具有抗肿瘤作用的与鞘氨醇激酶通路相关的抑制剂的研究进展.

Sphingosine kinase (SphK) is a lipid kinase, which has received extensive attention as an important enzyme in cancer biology. They are involved in the regulation of a variety of signaling pathways through the production of sphingosine-1-phosphate (S1P), which mediates a series of biological functions such as cell growth, differentiation, migration, and angiogenesis. Nowadays, the research of sphingosine kinase inhibitors is a hot topic worldwide, and with the analysis of the crystal structure of sphingosine kinase 1 (SphK1), more highly selective and highly active inhibitors have been developed. Herein, we have reviewed the sphingosine kinase-related inhibitors with anti-tumor and anti-inflammatory effects into four categories.