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Pharmacological Effects of FTY720 and its Derivatives
Current Topics in Medicinal Chemistry ( IF 3.4 ) Pub Date : 2024-01-05 , DOI: 10.2174/0115680266273421231222061620
Mengyuan Han 1 , Xiangran Liu 1 , Sendaer Hailati 1 , Nulibiya Maihemuti 1 , Nurbiya Nurahmat 1 , Dilihuma Dilimulati 1 , Alhar baishan 1 , Alifeiye Aikebaier 1 , Wenting Zhou 1 , Yan Pan 2
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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.

中文翻译:

FTY720及其衍生物的药理作用

FTY720 是源自子囊菌冬虫夏草的 1-磷酸鞘氨醇 (S1P) 类似物。FTY720作为一种新型免疫抑制剂,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的非磷酸化形式可通过抑制SPHK1(鞘氨醇激酶1)和激活PP2A(蛋白磷酸酶2A)以及多种细胞死亡途径,诱导细胞凋亡,增强化疗敏感性,抑制多种肿瘤的肿瘤转移。FTY720可在体外诱导中性粒细胞胞外陷阱中和并杀死病原体,从而发挥抗感染作用。目前,通过结构修饰已开发出一系列具有抗肿瘤、缓解气道高反应性等药理作用的FTY720衍生物。本文综述了FTY720及其衍生物的药理作用。
更新日期:2024-01-05
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