关键词: Anti-infection Anti-tumor Derivative FTY720 Immunosuppression Pharmacological effects.

Mesh : Fingolimod Hydrochloride / pharmacology chemistry Humans Animals Immunosuppressive Agents / pharmacology chemistry chemical synthesis Antineoplastic Agents / pharmacology chemistry Neoplasms / drug therapy pathology Apoptosis / drug effects

来  源:   DOI:10.2174/0115680266273421231222061620

Abstract:
FTY720 is an analog of sphingosine-1-phosphate (S1P) derived from the ascomycete Cordyceps sinensis. As a new immunosuppressant, FTY720 is widely used to treat multiple sclerosis. FTY720 binds to the S1P receptor after phosphorylation, thereby exerting immunosuppressive effects. The nonphosphorylated form of FTY720 can induce cell apoptosis, enhance chemotherapy sensitivity, and inhibit tumor metastasis of multiple tumors by inhibiting SPHK1 (sphingosine kinase 1) and activating PP2A (protein phosphatase 2A) and various cell death pathways. FTY720 can induce neutrophil extracellular traps to neutralize and kill pathogens in vitro, thus exerting anti- infective effects. At present, a series of FTY720 derivatives, which have pharmacological effects such as anti-tumor and alleviating airway hyperresponsiveness, have been developed through structural modification. This article reviews the pharmacological effects of FTY720 and its derivatives.
摘要:
FTY720是源自子囊虫草的鞘氨醇-1-磷酸(S1P)的类似物。作为一种新的免疫抑制剂,FTY720广泛用于治疗多发性硬化症。FTY720磷酸化后与S1P受体结合,从而发挥免疫抑制作用。FTY720的非磷酸化形式可以诱导细胞凋亡,增强化疗敏感性,并通过抑制SPHK1(鞘氨醇激酶1)和激活PP2A(蛋白磷酸酶2A)和各种细胞死亡途径来抑制多种肿瘤的肿瘤转移。FTY720在体外能诱导中性粒细胞胞外诱捕网中和杀灭病原菌,从而发挥抗感染作用。目前,一系列FTY720衍生物,具有抗肿瘤和缓解气道高反应性等药理作用,已经通过结构改性开发。本文综述了FTY720及其衍生物的药理作用。
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