Smith H J, Wyke S M, Tisdale M J
Pharmaceutical Sciences Research Institute, Aston University, Birmingham, B4 7ET, UK.
Br J Cancer. 2004 May 4;90(9):1850-7. doi: 10.1038/sj.bjc.6601767.
Proteolysis-inducing factor (PIF) is a sulphated glycoprotein produced by cachexia-inducing tumours, which initiates muscle protein degradation through an increased expression of the ubiquitin-proteasome proteolytic pathway. The role of kinase C (PKC) in PIF-induced proteasome expression has been studied in murine myotubes as a surrogate model of skeletal muscle. Proteasome expression induced by PIF was attenuated by 4alpha-phorbol 12-myristate 13-acetate (100 nM) and by the PKC inhibitors Ro31-8220 (10 microM), staurosporine (300 nM), calphostin C (300 nM) and Gö 6976 (200 microM). Proteolysis-inducing factor-induced activation of PKC(alpha), with translocation from the cytosol to the membrane at the same concentration as that inducing proteasome expression, and this effect was attenuated by calphostin C. Myotubes transfected with a constitutively active PKC(alpha) (pCO(2)) showed increased expression of proteasome activity, and a longer time course, compared with their wild-type counterparts. In contrast, myotubes transfected with a dominant-negative PKC(alpha) (pKS1), which showed no activation of PKC(alpha) in response to PIF, exhibited no increase in proteasome activity at any time point. Proteolysis-inducing factor-induced proteasome expression has been suggested to involve the transcription factor nuclear factor-kappaB (NF-kappaB), which may be activated through PKC. Proteolysis-inducing factor induced a decrease in cytosolic I-kappaBalpha and an increase in nuclear binding of NF-kappaB in pCO(2), but not in pKS1, and the effect in wild-type cells was attenuated by calphostin C, confirming that it was mediated through PKC. This suggests that PKC may be involved in the phosphorylation and degradation of I-kappaBalpha, induced by PIF, necessary for the release of NF-kappaB from its inactive cytosolic complex.
蛋白水解诱导因子(PIF)是一种由恶病质诱导肿瘤产生的硫酸化糖蛋白,它通过增加泛素-蛋白酶体蛋白水解途径的表达来启动肌肉蛋白降解。作为骨骼肌的替代模型,已在小鼠肌管中研究了蛋白激酶C(PKC)在PIF诱导的蛋白酶体表达中的作用。PIF诱导的蛋白酶体表达被4α-佛波醇12-肉豆蔻酸酯13-乙酸酯(100 nM)以及PKC抑制剂Ro31-8220(10 μM)、星形孢菌素(300 nM)、钙磷蛋白C(300 nM)和Gö 6976(200 μM)减弱。蛋白水解诱导因子诱导的PKC(α)激活,在与诱导蛋白酶体表达相同的浓度下从胞质溶胶转位到细胞膜,并且这种效应被钙磷蛋白C减弱。与野生型对应物相比,用组成型活性PKC(α)(pCO₂)转染的肌管显示蛋白酶体活性表达增加,且时间进程更长。相反,用显性负性PKC(α)(pKS1)转染的肌管,其对PIF无PKC(α)激活,在任何时间点均未表现出蛋白酶体活性增加。蛋白水解诱导因子诱导的蛋白酶体表达被认为涉及转录因子核因子-κB(NF-κB),其可能通过PKC激活。蛋白水解诱导因子在pCO₂中诱导胞质I-κBα减少和NF-κB核结合增加,但在pKS1中未出现,并且在野生型细胞中的效应被钙磷蛋白C减弱,证实其通过PKC介导。这表明PKC可能参与了PIF诱导的I-κBα的磷酸化和降解,这是NF-κB从其无活性的胞质复合物中释放所必需的。