新型鞘氨醇-1-磷酸受体选择性激动剂的研究进展

Advances in selective sphingosine-1-phosphate receptor subtype-1 agonists

自芬戈莫德(fingolimod,FTY720)发现以来,鞘氨醇-1-磷酸(S1P)受体受到研究者的广泛关注,但是在S1P受体的5种亚型(S1P1～S1P5)中,只有S1P1受体的激动剂可通过控制淋巴细胞的迁移而产生较强的免疫抑制效应。因此,寻找S1P1受体选择性激动剂,并研究其构效关系,具有非常重要的意义。本文主要对4类新型的S1P1受体激动剂的研究现状及构效关系进行综述。

Since fingolimod（FFY720） was found, sphingosine-l-phosphate （S1P） receptor has attracted the attention of sci- entists. Although five subtypes of S1P receptors, S1P1-S1P5 , are found, only the SIP1 receptor agonists can control the migration of lymphatic cells and show a strong immunosuppressive effect. Thus, it is very important to search for the S1P1 receptor-selective agonists and investigate their structure-activity relationships（SAR）. This paper focuses on the SAR and research advances in four types of new S1P1 receptor-selective agonists.