GSK3 beta-dependent phosphorylation of the alpha NAC coactivator regulates its nuclear translocation and proteasome-mediated degradation
Isabelle Quélo1, Omar Akhouayri, Josée Prud'homme
1Genetics Unit, Shriners Hospital for Children, Montréal, Québec, Canada H3G 1A6.
Abstract:
c-Jun is an immediate-early gene whose degradation by the proteasome pathway is required for an efficient transactivation. In this report, we demonstrated that the c-Jun coactivator, nascent polypeptide associated complex and coactivator alpha (alphaNAC) was also a target for degradation by the 26S proteasome. The proteasome inhibitor lactacystin increased the metabolic stability of alphaNAC in vivo, and lactacystin, MG-132, or epoxomicin treatment of cells induced nuclear translocation of alphaNAC. We have shown that the ubiquitous kinase glycogen synthase kinase 3beta (GSK3beta) directly phosphorylated alphaNAC in vitro and in vivo. Inhibition of the endogenous GSKappa3beta activity resulted in the stabilization of this coactivator in vivo. We identified the phosphoacceptor site in the C-terminal end of the coactivator, on position threonine 159. We demonstrated that the inhibition of GSK3beta activity by treatment of cells with the inhibitor 5-iodo-indirubin-3'-monoxime, as well as with a dominant-negative GSK3beta mutant, induced the accumulation of alphaNAC in the nuclei of cells. Mutation of the GSK3beta phosphoacceptor site on alphaNAC induced a significant increase of its coactivation potency. We conclude that GSK3beta-dependent phosphorylation of alphaNAC was the signal that directed the protein to the proteasome. The accumulation of alphaNAC caused by the inhibition of the proteasome pathway or the activity of GSK3beta contributes to its nuclear translocation and impacts on its coactivating function.
Insights
The proteasome degrades the alphaNAC coactivator, a process regulated by glycogen synthase kinase 3beta (GSK3beta) phosphorylation. Inhibiting GSK3beta or the proteasome stabilizes alphaNAC, promoting its nuclear translocation and enhancing its coactivation function.
Area of Science:
- Molecular Biology
- Cell Biology
- Biochemistry
Background:
- c-Jun transactivation requires proteasomal degradation.
- The nascent polypeptide-associated complex and coactivator alpha (alphaNAC) is a c-Jun coactivator.
- The role of alphaNAC degradation in gene regulation is not fully understood.
Purpose of the Study:
- To investigate the role of the proteasome pathway in alphaNAC stability and function.
- To identify the regulatory mechanisms controlling alphaNAC degradation.
- To determine the impact of alphaNAC stability on its coactivator activity.
Main Methods:
- Proteasome inhibition using lactacystin, MG-132, and epoxomicin.
- In vitro and in vivo phosphorylation assays using glycogen synthase kinase 3beta (GSK3beta).
- Site-directed mutagenesis to identify the phosphoacceptor site (Threonine 159).
- Dominant-negative GSK3beta mutants and specific inhibitors (5-iodo-indirubin-3'-monoxime).
Main Results:
- Proteasome inhibitors increased alphaNAC metabolic stability and induced nuclear translocation.
- GSK3beta directly phosphorylated alphaNAC in vitro and in vivo.
- Inhibition of GSK3beta activity stabilized alphaNAC and promoted its nuclear accumulation.
- Mutation of the GSK3beta phosphorylation site enhanced alphaNAC coactivation potency.
Conclusions:
- GSK3beta-dependent phosphorylation targets alphaNAC for proteasomal degradation.
- Inhibition of either GSK3beta or the proteasome leads to alphaNAC accumulation in the nucleus.
- AlphaNAC nuclear translocation and enhanced coactivation are consequences of its stabilization.
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