中文摘要：

鞘胺醇－1－磷酸（SIP）是调节细胞内外多种生物学功能的重要信号分子。S1P可通过结合5种G蛋白偶联受体亚型（S1PR1－5）介导多重下游信号通路产生相关的细胞生理功能，其中激动S1PR1可以达到调节免疫的作用。新型S1PRl激动剂芬戈莫德（Fingolimod，FTY-720）已完成临床研究成为自身免疫性疾病——多发性硬化症的治疗药物。选择性S1PR。激动剂的研究己成为发现免疫性疾病治疗药物的热点。本文总结了近年来该领域的研究进展，着重介绍S1PR1激动剂的结构类型和构效关系研究，并探讨了此类激动剂的发展方向。

英文摘要：

Sphingosine-l-phosphate （S1P） is a lysophospholipid signaling molecule that regulates important biological functions in both intracellular and extracellular compartments. It interacts with five G protein-coupled receptors subtypes （S1PR1 5） to generate multiple downstream signaling. Activation of S1PR1 has been validated to be involved in the process of immune modulation. Fingolimod （FTY720）, the novel S 1PRI agonist, has been approved for the treatment of multiple sclerosis in clinical trials. The study towards discovery of selective S 1PR1 agonists has become hot spot for immunological diseases. This article summarized the research progress of S1PR1 agonists, emphasizing their structure types, structure-activity relationship and direction of development.