PRT318对胶原诱导人血小板Syk磷酸化的影响

发布时间：2018-05-25 00:33

  本文选题：PRT + 胶原　； 参考：《中国现代医学杂志》2017年09期

【摘要】：目的观察脾酪氨酸激酶(Syk)抑制剂PRT060318(PRT318)在体外对人血小板聚集率及Syk磷酸化的影响。方法采用比浊法测定PRT318对胶原、二磷酸腺苷(ADP)及花生四烯酸(AA)诱导的人血小板聚集率的影响;运用Western blot检测Syk525/6磷酸化水平。结果 Syk特异性抑制剂PRT318可抑制胶原诱导的人血小板聚集率,但对ADP或AA诱导的人血小板聚集率无影响。在蛋白水平上PRT318可促进人血小板在胶原诱导下Syk525/6磷酸化水平升高。酪氨酸蛋白激酶抑制剂PP2可抑制胶原诱导的人血小板聚集,降低人血小板在胶原诱导下Syk525/6磷酸化水平,并可阻断胶原诱导下PRT318促Syk525/6磷酸化作用。结论 PRT318对胶原诱导的血小板聚集具有抑制作用,并能促进胶原诱导的血小板膜受体糖蛋白VI信号通路上Syk525/6磷酸化,提示PRT318可能通过作用于Syk525/6磷酸化而抑制血小板聚集。
[Abstract]:Objective to observe the effect of spleen tyrosine kinase Syk inhibitor PRT060318- PRT318 on human platelet aggregation and Syk phosphorylation in vitro. Methods the effect of PRT318 on the platelet aggregation induced by collagen, adenosine diphosphate and arachidonic acid was determined by turbidimetry, and the phosphorylation level of Syk525/6 was detected by Western blot. Results PRT318, a specific inhibitor of Syk, could inhibit human platelet aggregation induced by collagen, but had no effect on ADP or AA induced platelet aggregation. At the protein level, PRT318 promoted the increase of Syk525/6 phosphorylation in human platelets induced by collagen. Tyrosine protein kinase inhibitor (PP2) can inhibit collagen-induced human platelet aggregation, decrease the level of Syk525/6 phosphorylation induced by collagen, and block the collagen-induced Syk525/6 phosphorylation of PRT318. Conclusion PRT318 can inhibit platelet aggregation induced by collagen and promote Syk525/6 phosphorylation in collagen induced platelet membrane receptor glycoprotein VI signaling pathway, suggesting that PRT318 may inhibit platelet aggregation by acting on Syk525/6 phosphorylation.
【作者单位】： 河南中医药大学细胞成像实验室;河南中医药大学心血管病研究所;
【基金】：国家自然科学基金(No:81072968) 教育部留学回国人员科研启动基金[No:教外司(20011568)] 河南省重点科技攻关项目(No:102102310334)
【分类号】：R446.6
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本文编号：1931294