From the Department of Pharmacology, Vanderbilt University Medical Center, Nashville, Tennessee 37232-6600.
J Biol Chem. 2014 Feb 14;289(7):4219-32. doi: 10.1074/jbc.M113.518514. Epub 2013 Dec 26.
Serine/threonine protein phosphatase 5 (PP5, PPP5C) is known to interact with the chaperonin heat shock protein 90 (HSP90) and is involved in the regulation of multiple cellular signaling cascades that control diverse cellular processes, such as cell growth, differentiation, proliferation, motility, and apoptosis. Here, we identify PP5 in stable complexes with extracellular signal-regulated kinases (ERKs). Studies using mutant proteins reveal that the formation of PP5·ERK1 and PP5·ERK2 complexes partially depends on HSP90 binding to PP5 but does not require PP5 or ERK1/2 activity. However, PP5 and ERK activity regulates the phosphorylation state of Raf1 kinase, an upstream activator of ERK signaling. Whereas expression of constitutively active Rac1 promotes the assembly of PP5·ERK1/2 complexes, acute activation of ERK1/2 fails to influence the phosphatase-kinase interaction. Introduction of oncogenic HRas (HRas(V12)) has no effect on PP5-ERK1 binding but selectively decreases the interaction of PP5 with ERK2, in a manner that is independent of PP5 and MAPK/ERK kinase (MEK) activity, yet paradoxically requires ERK2 activity. Additional studies conducted with oncogenic variants of KRas4B reveal that KRas(L61), but not KRas(V12), also decreases the PP5-ERK2 interaction. The expression of wild type HRas or KRas proteins fails to reduce PP5-ERK2 binding, indicating that the effect is specific to HRas(V12) and KRas(L61) gain-of-function mutations. These findings reveal a novel, differential responsiveness of PP5-ERK1 and PP5-ERK2 interactions to select oncogenic Ras variants and also support a role for PP5·ERK complexes in regulating the feedback phosphorylation of PP5-associated Raf1.
丝氨酸/苏氨酸蛋白磷酸酶 5(PP5,PPP5C)已知与伴侣蛋白热休克蛋白 90(HSP90)相互作用,并参与调节多个细胞信号级联反应,这些级联反应控制着多种细胞过程,如细胞生长、分化、增殖、运动和凋亡。在这里,我们鉴定出与细胞外信号调节激酶(ERK)稳定结合的 PP5。使用突变蛋白的研究表明,PP5·ERK1 和 PP5·ERK2 复合物的形成部分依赖于 HSP90 与 PP5 的结合,但不依赖于 PP5 或 ERK1/2 的活性。然而,PP5 和 ERK 活性调节 Raf1 激酶的磷酸化状态,Raf1 激酶是 ERK 信号的上游激活剂。虽然组成性激活的 Rac1 促进 PP5·ERK1/2 复合物的组装,但 ERK1/2 的急性激活不能影响磷酸酶-激酶相互作用。致癌 HRas(HRas(V12)) 的表达对 PP5-ERK1 结合没有影响,但选择性地降低 PP5 与 ERK2 的相互作用,这种方式独立于 PP5 和 MAPK/ERK 激酶(MEK)活性,但矛盾的是需要 ERK2 活性。对致癌 KRas4B 变体进行的进一步研究表明,KRas(L61),而不是 KRas(V12),也降低了 PP5-ERK2 的相互作用。野生型 HRas 或 KRas 蛋白的表达不能降低 PP5-ERK2 的结合,表明这种效应是 HRas(V12)和 KRas(L61)功能获得性突变所特有的。这些发现揭示了 PP5-ERK1 和 PP5-ERK2 相互作用对选择致癌 Ras 变体的新型、差异反应性,并支持 PP5·ERK 复合物在调节与 PP5 相关的 Raf1 的反馈磷酸化中的作用。