Synthesis of Phosphatidylserine and Its Stereoisomers: Their Role in Activation of Blood Coagulation,ACS Medicinal Chemistry Letters

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Synthesis of Phosphatidylserine and Its Stereoisomers: Their Role in Activation of Blood Coagulation
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2018-04-12 00:00:00 , DOI: 10.1021/acsmedchemlett.8b00008
Suman Mallik ₁ , Ramesh Prasad ₁ , Anindita Bhattacharya ₁ , Prosenjit Sen ₁

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Natural phosphatidylserine (PS), which contains two chiral centers, enhances blood coagulation. However, the process by which PS enhanced blood coagulation is not completely understood. An efficient and flexible synthetic route has been developed to synthesize all of the possible stereoisomers of PS. In this study, we examined the role of PS chiral centers in modulating the activity of the tissue factor (TF)-factor VIIa coagulation initiation complex. Full length TF was relipidated with phosphatidylcholine, and the synthesized PS isomers were individually used to estimate the procoagulant activity of the TF-FVIIa complex via a FXa generation assay. The results revealed that the initiation complex activity was stereoselective and had increased sensitivity to the configuration of the PS glycerol backbone due to optimal protein–lipid interactions.

中文翻译：

磷脂酰丝氨酸及其立体异构体的合成：在凝血激活中的作用

包含两个手性中心的天然磷脂酰丝氨酸（PS）可增强血液凝结。但是，PS增强凝血的过程尚不完全清楚。已经开发出有效且灵活的合成路线来合成PS的所有可能的立体异构体。在这项研究中，我们检查了PS手性中心在调节组织因子（TF）-VIIa凝血起始复合物活性中的作用。全长TF用磷脂酰胆碱重新脂质化，合成的PS异构体分别用于通过FXa生成测定法评估TF-FVIIa复合物的促凝活性。结果表明，由于最佳的蛋白质-脂质相互作用，起始复合物的活性具有立体选择性，并且对PS甘油骨架的构型具有更高的敏感性。

更新日期：2018-04-12

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