Perander Maria, Aberg Espen, Johansen Bjarne, Dreyer Bo, Guldvik Ingrid J, Outzen Heidi, Keyse Stephen M, Seternes Ole-Morten
Department of Pharmacology, Institute of Medical Biology, University of Tromsø, N-9037 Tromsø, Norway.
Biochem J. 2008 May 1;411(3):613-22. doi: 10.1042/BJ20071369.
ERK (extracellular-signal-regulated kinase) 4 [MAPK (mitogen-activated protein kinase) 4] and ERK3 (MAPK6) are atypical MAPKs. One major difference between these proteins and the classical MAPKs is substitution of the conserved T-X-Y motif within the activation loop by a single phospho-acceptor site within an S-E-G motif. In the present study we report that Ser(186) of the S-E-G motif in ERK4 is phosphorylated in vivo. Kinase-dead ERK4 is also phosphorylated on Ser(186), indicating that an ERK4 kinase, rather than autophosphorylation, is responsible. Co-expression of MK5 [MAPK-activated protein kinase 5; also known as PRAK (p38-regulated/activated kinase)], a physiological target of ERK4, increases phosphorylation of Ser(186). This is not dependent on MK5 activity, but does require interaction between ERK4 and MK5 suggesting that MK5 binding either prevents ERK4 dephosphorylation or facilitates ERK4 kinase activity. ERK4 mutants in which Ser(186) is replaced with either an alanine residue or a phospho-mimetic residue (glutamate) are unable to activate MK5 and Ser(186) is also required for cytoplasmic anchoring of MK5. Both defects seem to reflect an impaired ability of the ERK4 mutants to interact with MK5. We find that there are at least two endogenous pools of wild-type ERK4. One form exhibits reduced mobility when analysed using SDS/PAGE. This is due to MK5-dependent phosphorylation and only this retarded ERK4 species is both phosphorylated on Ser(186) and co-immunoprecipitates with wild-type MK5. We conclude that binding between ERK4 and MK5 facilitates phosphorylation of Ser(186) and stabilization of the ERK4-MK5 complex. This results in phosphorylation and activation of MK5, which in turn phosphorylates ERK4 on sites other than Ser(186) resulting in the observed mobility shift.
细胞外信号调节激酶(ERK)4[丝裂原活化蛋白激酶(MAPK)4]和ERK3(MAPK6)属于非典型丝裂原活化蛋白激酶。这些蛋白与经典丝裂原活化蛋白激酶的一个主要区别在于,其激活环内保守的T-X-Y基序被S-E-G基序内的单个磷酸化受体位点所取代。在本研究中,我们报告ERK4的S-E-G基序中的Ser(186)在体内被磷酸化。激酶失活的ERK4在Ser(186)位点也被磷酸化,这表明是ERK4激酶而非自身磷酸化起作用。ERK4的生理靶点MK5[MAPK激活的蛋白激酶5;也称为PRAK(p38调节/激活的激酶)]的共表达增加了Ser(186)的磷酸化。这并不依赖于MK5的活性,但确实需要ERK4与MK5之间的相互作用,这表明MK5的结合要么阻止ERK4的去磷酸化,要么促进ERK4激酶的活性。将Ser(186)替换为丙氨酸残基或磷酸模拟残基(谷氨酸)的ERK4突变体无法激活MK5,并且Ser(186)对于MK5的细胞质锚定也是必需的。这两个缺陷似乎都反映了ERK4突变体与MK5相互作用的能力受损。我们发现野生型ERK4至少有两个内源性池。其中一种形式在使用SDS/PAGE分析时迁移率降低。这是由于MK5依赖性磷酸化,只有这种迁移受阻的ERK4物种在Ser(186)位点被磷酸化并与野生型MK5共免疫沉淀。我们得出结论,ERK4与MK5之间的结合促进了Ser(186)的磷酸化以及ERK4-MK5复合物的稳定。这导致MK5的磷酸化和激活,进而使ERK4在Ser(186)以外的位点磷酸化,导致观察到的迁移率变化。