Sah V P, Hoshijima M, Chien K R, Brown J H
Department of Pharmacology and Graduate Program in Biomedical Sciences, University of California, San Diego, La Jolla, CA 92093, USA.
J Biol Chem. 1996 Dec 6;271(49):31185-90. doi: 10.1074/jbc.271.49.31185.
G protein-coupled receptor agonists initiate a cascade of signaling events in neonatal rat ventricular myocytes that culminates in changes in gene expression and cell growth characteristic of hypertrophy. These responses have been previously shown to be dependent on Gq and Ras. Rho, a member of the Ras superfamily of GTPases, regulates cytoskeletal rearrangement and transcriptional activation of the c-fos serum response element. Immunofluorescence staining of cardiomyocytes shows that Rho is present and predominantly cytosolic. We used two inhibitors of Rho function, dominant negative N19RhoA and Clostridium botulinum C3 transferase, to examine the possible requirement for Rho in alpha1-adrenergic receptor-mediated hypertrophy. Both inhibitors markedly attenuated atrial natriuretic factor (ANF) reporter gene expression induced by alpha1-adrenergic receptor stimulation with phenylephrine, and virtually abolished the increase in ANF reporter gene expression induced by GTPase-deficient Galphaq. These effects were reproduced with the myosin light chain-2 reporter gene. Notably, N19RhoA did not block the ability of activated Ras to induce ANF and myosin light chain-2 reporter gene expression. Furthermore, activation of the extracellular signal-regulated kinase by phenylephrine was not blocked by N19RhoA, nor was it stimulated by an activated mutant of RhoA. Since activated RhoA and Ras produce a large synergistic effect on ANF-luciferase gene expression, we conclude that Rho functions in a pathway separate from but complementary to Ras. Our results provide direct evidence that Rho is an effector of Galphaq signaling and suggest for the first time that a low molecular weight GTPase other than Ras is involved in regulating myocardial cell growth and gene expression in response to heterotrimeric G protein-linked receptor activation.
G蛋白偶联受体激动剂在新生大鼠心室肌细胞中引发一系列信号事件,最终导致基因表达变化和肥大特征性的细胞生长。这些反应先前已被证明依赖于Gq和Ras。Rho是GTP酶Ras超家族的成员,可调节细胞骨架重排和c-fos血清反应元件的转录激活。心肌细胞的免疫荧光染色显示Rho存在且主要位于细胞质中。我们使用两种Rho功能抑制剂,显性负性N19RhoA和肉毒杆菌C3转移酶,来研究Rho在α1-肾上腺素能受体介导的肥大中的可能需求。两种抑制剂均显著减弱了苯肾上腺素刺激α1-肾上腺素能受体诱导的心房利钠因子(ANF)报告基因表达,并且几乎消除了GTP酶缺陷型Gαq诱导的ANF报告基因表达增加。肌球蛋白轻链-2报告基因也出现了这些效应。值得注意的是,N19RhoA并未阻断活化的Ras诱导ANF和肌球蛋白轻链-2报告基因表达的能力。此外,苯肾上腺素对细胞外信号调节激酶的激活未被N19RhoA阻断,RhoA的活化突变体也未刺激该激酶。由于活化的RhoA和Ras对ANF-荧光素酶基因表达产生很大的协同效应,我们得出结论,Rho在与Ras分开但互补的途径中发挥作用。我们的结果提供了直接证据,表明Rho是Gαq信号传导的效应器,并首次表明除Ras外的一种低分子量GTP酶参与调节心肌细胞生长和基因表达以响应异三聚体G蛋白偶联受体激活。