Proteinase-activated receptors:: a growing family of heptahelical receptors for thrombin, trypsin and tryptase
Proteinase-activated receptors:: a growing family of heptahelical receptors for thrombin, trypsin and tryptase
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DOI：
10.1042/bst0270246
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发表时间：
1999-02-01
影响因子：
3.9
通讯作者：
Bunnett, NW
中科院分区：
文献类型：
--
作者：
Dáry, O;Bunnett, NW
尽管蛋白酶通常作为降解酶发挥作用，但某些酶具有通过新的和不断增长的G蛋白偶联受体（GPCR）家族介导的生物活性（综述于[1]）。最好的例子是凝血酶，其活性与其在凝血级联中的作用不同。在1991年，Coughlin和同事分离了编码GPCR的cDNA，该GPCR介导凝血酶的许多细胞效应[Z]。最初命名为凝血酶受体，随后在发现相关受体后更名为蛋白酶激活受体1（PAR-1）。凝血酶激活PAR-1基因敲除小鼠的血小板，但对这些动物的成纤维细胞没有影响，这证明了添加凝血酶可以激活血小板。
Although proteases usually function as degradative enzymes, certain enzymes have biological activity that is mediated through a new and growing family of G-protein-coupled receptors (GPCRs)(reviewed in [l]). The best example is thrombin, which has activity distinct from its role in the coagulation cascade. In 1991, Coughlin and colleagues isolated a cDNA encoding a GPCR that mediates many of thrombin's cellular effects [Z]. Initially named the thrombin receptor, it was subsequently renamed proteinase-activated receptor 1 (PAR-1) after the discovery of related receptors. Thrombin activated platelets from PAR-1 knockout mice, but had no effect on fibroblasts from these animals, proving that addi-