本文選題：PRT + 膠原　； 參考：《中國現(xiàn)代醫(yī)學雜志》2017年09期

【摘要】：目的觀察脾酪氨酸激酶(Syk)抑制劑PRT060318(PRT318)在體外對人血小板聚集率及Syk磷酸化的影響。方法采用比濁法測定PRT318對膠原、二磷酸腺苷(ADP)及花生四烯酸(AA)誘導(dǎo)的人血小板聚集率的影響;運用Western blot檢測Syk525/6磷酸化水平。結(jié)果 Syk特異性抑制劑PRT318可抑制膠原誘導(dǎo)的人血小板聚集率,但對ADP或AA誘導(dǎo)的人血小板聚集率無影響。在蛋白水平上PRT318可促進人血小板在膠原誘導(dǎo)下Syk525/6磷酸化水平升高。酪氨酸蛋白激酶抑制劑PP2可抑制膠原誘導(dǎo)的人血小板聚集,降低人血小板在膠原誘導(dǎo)下Syk525/6磷酸化水平,并可阻斷膠原誘導(dǎo)下PRT318促Syk525/6磷酸化作用。結(jié)論 PRT318對膠原誘導(dǎo)的血小板聚集具有抑制作用,并能促進膠原誘導(dǎo)的血小板膜受體糖蛋白VI信號通路上Syk525/6磷酸化,提示PRT318可能通過作用于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.
【作者單位】： 河南中醫(yī)藥大學細胞成像實驗室;河南中醫(yī)藥大學心血管病研究所;
【基金】：國家自然科學基金(No:81072968) 教育部留學回國人員科研啟動基金[No:教外司(20011568)] 河南省重點科技攻關(guān)項目(No:102102310334)
【分類號】：R446.6
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本文編號：1931294