鞘氨醇激酶的相关抑制剂研究进展  

Progress on the research of sphingosine kinase related inhibitors

作　　者：陈海蛟 柴会宁 刘波[1,2,3,4] 姚庆强[1,2,3,4] CHEN Haijiao;CHAI Huining;LIU Bo;YAO Qingqiang(School of Medicine and Life Sciences,University of Jinan-Shandong Academy of Medical Sciences,Jinan 250200,Shandong,China;Institute of Materia Medica,Shandong Academy of Medical Sciences,Jinan 250062,Shandong,China;Key Laboratory for Biotech-Drugs Ministry of Health,Jinan 250062,Shandong,China;Key Laboratory for Rare & Uncommon Diseases of Shandong Province,Jinan 250062,Shandong,China)

机构地区：[1]济南大学山东省医学科学院医学与生命科学学院,山东济南250200 [2]山东省医学科学院药物研究所,山东济南250062 [3]国家卫生部生物技术药物重点实验室,山东济南250062 [4]山东省罕少见病重点实验室,山东济南250062

出　　处：《化学研究》2019年第3期310-316,共7页Chemical Research

基　　金：国家自然科学青年科学基金(21801158)

摘　　要：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.

关 键 词：鞘氨醇激酶 鞘氨醇-1-磷酸 鞘氨醇激酶抑制剂 配体结合口袋 ATP结合口袋 

分 类 号：O625[理学—有机化学]