Rosing J, Maurissen L F A, Tchaikovski S N, Tans G, Hackeng T M
Department of Biochemistry, Cardiovascular Research Institute Maastricht, Maastricht University, Maastricht, The Netherlands.
Thromb Res. 2008;122 Suppl 1:S60-3. doi: 10.1016/S0049-3848(08)70021-5.
Protein S is a vitamin K-dependent protein that acts as a cofactor of the anticoagulant protein APC. However, protein S also exhibits anticoagulant activity in the absence of APC. Thrombin generation experiments in normal plasma and in plasma deficient in tissue factor pathway inhibitor (TFPI) and/or protein S demonstrated that protein S stimulates the inhibition of TF by TFPI. Kinetic analysis in model systems containing purified proteins showed that protein S enhances the formation of the binary FXa:TFPI complex by reducing the Ki of TFPI from approximately 4 nM to approximately 0.5 nM. Enhancement of inhibitory activity of TFPI by protein S is only observed with full-length TFPI and in the presence of a negatively charged phospholipid surface. The Ki decrease brings the TFPI concentration necessary for FXa:TFPI complex formation within range of the plasma TFPI concentration which increases FXa:TFPI complex formation and accelerates feedback inhibition of the TF pathway by enhancing the formation of the quaternary TFPI:FXa:TF:FVIIa complex. Thus, protein S is not only a cofactor of APC, but also of TFPI. A reduced TFPI cofactor activity may contribute to the increased risk of venous thrombosis in protein-S deficient individuals. Using calibrated automated thrombography we have developed two assays that enable quantification of the functional activity of the TFPI/protein S system in plasma. These assays show that the activity of the TFPI/protein S system is greatly impaired in oral contraceptive users.
蛋白S是一种维生素K依赖蛋白,作为抗凝蛋白活化蛋白C(APC)的辅因子发挥作用。然而,在没有APC的情况下,蛋白S也表现出抗凝活性。在正常血浆以及缺乏组织因子途径抑制物(TFPI)和/或蛋白S的血浆中进行的凝血酶生成实验表明,蛋白S能刺激TFPI对组织因子(TF)的抑制作用。在含有纯化蛋白的模型系统中进行的动力学分析表明,蛋白S通过将TFPI的抑制常数(Ki)从约4 nM降低至约0.5 nM,增强了二元因子Xa(FXa):TFPI复合物的形成。只有在全长TFPI存在且有带负电荷的磷脂表面时,才能观察到蛋白S增强TFPI的抑制活性。Ki的降低使FXa:TFPI复合物形成所需的TFPI浓度处于血浆TFPI浓度范围内,这增加了FXa:TFPI复合物的形成,并通过增强四元TFPI:FXa:TF:凝血因子VIIa(FVIIa)复合物的形成加速了TF途径的反馈抑制。因此,蛋白S不仅是APC的辅因子,也是TFPI的辅因子。TFPI辅因子活性降低可能导致蛋白S缺乏个体静脉血栓形成风险增加。我们使用校准自动血栓形成检测法开发了两种检测方法,可对血浆中TFPI/蛋白S系统的功能活性进行定量。这些检测方法表明,口服避孕药使用者中TFPI/蛋白S系统的活性严重受损。