Turner J S, Redpath G T, Humphries J E, Gonias S L, Vandenberg S R
Department of Pathology (Neuropathology), University of Virginia Health Sciences Center, Charlottesville 22908.
Biochem J. 1994 Jan 1;297 ( Pt 1)(Pt 1):175-9. doi: 10.1042/bj2970175.
Extracellular proteinases may be selectively targeted to cell surfaces by specific receptors or binding sites. In previous studies, we have characterized cellular binding sites for plasminogen and plasmin on rat C6 glioma cells. In this investigation, we studied the response of C6 cells to alpha-thrombin and plasmin by measuring the rapid kinetics of free intracellular Ca2+ concentrations ([Ca2+]i). Thrombin produced a strong, concentration-dependent rise in [Ca2+]i with an onset within 3 s and peak levels achieved in less than 10 s. A similar response was also evoked by an SFLLRN-containing thrombin-agonist peptide. C6 cells did not respond to plasmin (25 nM-1.5 microM). By contrast, pretreatment of C6 cells with 100 nM plasmin significantly inhibited the [Ca2+]i response to thrombin and the thrombin-agonist peptide. The peak [Ca2+]i response to thrombin, in cells pretreated with plasmin, was reduced by approx. 50%. The effect of plasmin on the cellular response to thrombin was selective, as pretreatment of the cells with plasmin did not affect the [Ca2+]i response to platelet-activating factor. Di-isopropylphosphorylplasmin and plasminogen did not inhibit the cellular response to thrombin, indicating that plasmin activity is required and that occupancy of cellular plasmin(ogen)-binding sites alone is insufficient. These studies demonstrate that plasmin does not directly induce a response in C6 cells, but may affect cellular function by specifically modulating the thrombin response.
细胞外蛋白酶可通过特定受体或结合位点选择性地靶向细胞表面。在先前的研究中,我们已经对大鼠C6胶质瘤细胞上纤溶酶原和纤溶酶的细胞结合位点进行了表征。在本研究中,我们通过测量细胞内游离钙离子浓度([Ca2+]i)的快速动力学,研究了C6细胞对α-凝血酶和纤溶酶的反应。凝血酶使[Ca2+]i产生强烈的、浓度依赖性升高,在3秒内开始,不到10秒达到峰值水平。含SFLLRN的凝血酶激动剂肽也能引起类似反应。C6细胞对纤溶酶(25 nM - 1.5 μM)无反应。相比之下,用100 nM纤溶酶预处理C6细胞可显著抑制其对凝血酶和凝血酶激动剂肽的[Ca2+]i反应。在用纤溶酶预处理的细胞中,对凝血酶的[Ca2+]i峰值反应降低了约50%。纤溶酶对细胞对凝血酶反应的影响具有选择性,因为用纤溶酶预处理细胞并不影响其对血小板活化因子的[Ca2+]i反应。二异丙基磷酰纤溶酶和纤溶酶原不能抑制细胞对凝血酶的反应,表明需要纤溶酶活性,仅占据细胞纤溶酶(原)结合位点是不够的。这些研究表明,纤溶酶不会直接在C6细胞中诱导反应,但可能通过特异性调节凝血酶反应来影响细胞功能。