Induction of vascular smooth muscle cell growth by selective activation of the thrombin receptor Effect of heparin
Induction of vascular smooth muscle cell growth by selective activation of the thrombin receptor Effect of heparin
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通过选择性激活凝血酶受体诱导血管平滑肌细胞生长 肝素的作用
DOI：
10.1016/0014-5793(92)81237-g
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发表时间：
1992
期刊：
影响因子：
3.5
通讯作者：
F. Dol
中科院分区：
文献类型：
--
作者：
J. Herbert;I. Lamarche;F. Dol
合成肽SFLLRNPNDKYEPF最近被描述为模拟凝血酶受体裂解产生的新氨基末端的肽，因此充当凝血酶受体的激动剂。该肽对兔动脉平滑肌细胞（SMC）有较强的促有丝分裂活性，其活性与天然α-凝血酶相当。这两种化合物刺激增殖的生长停滞的SMC与半最大促有丝分裂反应在1 nM。NAPAP是凝血酶酶活性的合成抑制剂，特异性抑制凝血酶诱导的SMC生长（IC 50 = 0.35 ± 0.04 μM），但对激动剂肽的促有丝分裂作用无影响。因此，这些结果表明α-凝血酶对SMC的促有丝分裂作用与其酯酶活性密切相关。肝素抑制胎牛血清诱导的SMC生长，但对凝血酶诱导的SMC生长没有影响，但强烈降低激动剂肽的促有丝分裂作用（IC 50 = 32 ± 5μ/ml）。这种效应与肝素的抗凝活性无关，但高度依赖于分子质量和分子的全局电荷，并且还观察到其他硫酸化多糖，如戊聚糖多硫酸酯。
The synthetic peptide, SFLLRNPNDKYEPF, has been recently described as a peptide mimicking the new amino-terminus created by cleavage of the thrombin receptor, therefore acting as an agonist of the thrombin receptor. This peptide was a potent mitogen for rabbit arterial smooth muscle cells (SMC) and exhibited the same activity as that of native α-thrombin. Both compounds stimulated the proliferation of growth-arrested SMCs with half-maximum mitogenic responses at 1 nM. NAPAP, a synthetic inhibitor of the enzymatic activity of thrombin, specifically inhibited thrombin-induced SMC growth (IC50= 0.35 ± 0.04 μM) but was without effect on the mitogenic effect of the agonist peptide. These results therefore demonstrate that the mitogenic effect of α-thrombin for SMCs is intimately linked to its esterolytic activity. Heparin, which inhibited fetal calf serum-induced SMC growth, was without effect on thrombin-induced SMC growth but strongly reduced the mitogenic effect of the agonist peptide (IC50= 32 ± 5μ/ml). This effect was not related to the anti-coagulant activity of heparin but was highly dependent on molecular mass and on the global charge of the molecule and was also observed for other sulphated polysaccharides such as pentosan polysulphate.
大鼠血管平滑肌细胞中凝血酶信号转导机制。
DOI：
--
发表时间：
1990
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
Berk,BC;Taubman,MB;CragoeJr,EJ;Fenton2nd,JW;Griendling,KK
通讯作者：
Griendling,KK
血管平滑肌细胞中 Na /H 交换器的凝血酶激活。
DOI：
--
发表时间：
1987
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
Huang,CL;Cogan,MG;CragoeJr,EJ;Ives,HE
通讯作者：
Ives,HE