Zohn I E, Yu H, Li X, Cox A D, Earp H S
Department of Pharmacology, University of North Carolina at Chapel Hill 27599, USA.
Mol Cell Biol. 1995 Nov;15(11):6160-8. doi: 10.1128/MCB.15.11.6160.
In GN4 rat liver epithelial cells, angiotensin II (Ang II) and other agonists which activate phospholipase C stimulate tyrosine kinase activity in a calcium-dependent, protein kinase C (PKC)-independent manner. Since Ang II also produces a proliferative response in these cells, we investigated downstream signaling elements traditionally linked to growth control by tyrosine kinases. First, Ang II, like epidermal growth factor (EGF), stimulated AP-1 binding activity in a PKC-independent manner. Because increases in AP-1 can reflect induction of c-Jun and c-Fos, we examined the activity of the mitogen-activated protein (MAP) kinase family members Erk-1 and -2 and the c-Jun N-terminal kinase (JNK), which are known to influence c-Jun and c-Fos transcription. Ang II stimulated MAP kinase (MAPK) activity but only approximately 50% as effectively as EGF; again, these effects were independent of PKC. Ang II also produced a 50- to 200-fold activation of JNK in a PKC-independent manner. Unlike its smaller effect on MAPK, Ang II was approximately four- to sixfold more potent in activating JNK than EGF was. Although others had reported a lack of calcium ionophore-stimulated JNK activity in lymphocytes and several other cell lines, we examined the role of calcium in GN4 cells. The following results suggest that JNK activation in rat liver epithelial cells is at least partially Ca(2+) dependent: (i) norepinephrine and vasopressin hormones that increase inositol 1,4,5-triphosphate stimulated JNK; (ii) both thapsigargin, a compound that produces an intracellular Ca(2+) signal, and Ca(2+) ionophores stimulated a dramatic increase in JNK activity (up to 200-fold); (iii) extracellular Ca(2+) chelation with ethylene glycol tetraacetic acid (EGTA) inhibited JNK activation by ionophore and intracellular chelation with 1,2-bis-(o-aminophenoxy)-ethane-N,N,N',N'-tetraacetic acid tetraacetoxymethyl-ester (BAPTA-AM) partially inhibited JNK activation by Ang II or thapsigargin; and (iv) JNK activation by Ang II was inhibited by pretreatment of cells with thapsigargin and EGTA, a procedure which depletes intracellular Ca(2+) stores. JNK activation following Ang II stimulation did not involve calmodulin; either W-7 nor calmidizolium, in concentrations sufficient to inhibit Ca(2+)/calmodulin-dependent kinase II, blocked JNK activation by Ang II. In contrast, genistein, in concentrations sufficient to inhibit Ca(2+)-dependent tyrosine phosphorylation, prevented Ang II and thapsigargin-induced JNK activation. In summary, in GN4 rat liver epithelial cells, Ang II stimulates JNK via a novel Ca(2+)-dependent pathway. The inhibition by genistein suggest that Ca(2+)-dependent tyrosine phosphorylation may modulate the JNK pathway in a cell type-specific manner, particularly in cells with a readily detectable Ca(2+)-regulated tyrosine kinase.
在GN4大鼠肝上皮细胞中,血管紧张素II(Ang II)和其他激活磷脂酶C的激动剂以钙依赖性、不依赖蛋白激酶C(PKC)的方式刺激酪氨酸激酶活性。由于Ang II在这些细胞中也产生增殖反应,我们研究了传统上与酪氨酸激酶介导的生长控制相关的下游信号元件。首先,Ang II与表皮生长因子(EGF)一样,以不依赖PKC的方式刺激AP-1结合活性。因为AP-1的增加可以反映c-Jun和c-Fos的诱导,我们检测了丝裂原活化蛋白(MAP)激酶家族成员Erk-1和-2以及c-Jun氨基末端激酶(JNK)的活性,已知它们会影响c-Jun和c-Fos转录。Ang II刺激丝裂原活化蛋白激酶(MAPK)活性,但效力仅约为EGF的50%;同样,这些作用不依赖于PKC。Ang II还以不依赖PKC的方式使JNK激活50至200倍。与其对MAPK的较小作用不同,Ang II激活JNK的效力比EGF强约四至六倍。尽管其他人曾报道钙离子载体在淋巴细胞和其他几种细胞系中不能刺激JNK活性,但我们研究了钙离子在GN4细胞中的作用。以下结果表明大鼠肝上皮细胞中JNK的激活至少部分依赖于Ca(2+):(i)增加肌醇1,4,5-三磷酸的去甲肾上腺素和血管加压素激素刺激JNK;(ii)毒胡萝卜素(一种产生细胞内Ca(2+)信号的化合物)和Ca(2+)离子载体均刺激JNK活性显著增加(高达200倍);(iii)用乙二醇双四乙酸(EGTA)进行细胞外Ca(2+)螯合可抑制离子载体诱导的JNK激活,用1,2-双(邻氨基苯氧基)乙烷-N,N,N',N'-四乙酸四乙酰甲酯(BAPTA-AM)进行细胞内螯合可部分抑制Ang II或毒胡萝卜素诱导的JNK激活;(iv)用毒胡萝卜素和EGTA预处理细胞(该过程耗尽细胞内Ca(2+)储存)可抑制Ang II诱导的JNK激活。Ang II刺激后JNK的激活不涉及钙调蛋白;W-7和氯米帕明在足以抑制Ca(2+)/钙调蛋白依赖性激酶II的浓度下,均不能阻断Ang II诱导的JNK激活。相反,金雀异黄素在足以抑制Ca(2+)依赖性酪氨酸磷酸化的浓度下,可阻止Ang II和毒胡萝卜素诱导的JNK激活。总之,在GN4大鼠肝上皮细胞中,Ang II通过一条新的Ca(2+)依赖性途径刺激JNK。金雀异黄素的抑制作用表明Ca(2+)依赖性酪氨酸磷酸化可能以细胞类型特异性方式调节JNK途径,特别是在具有易于检测的Ca(2+)调节酪氨酸激酶的细胞中。