Phosphorylation of intestine-specific homeobox by ERK1 modulates
oncogenic activity and sorafenib resistance
Abstract
Nuclear translocation regulated by phosphorylation is a key step in
providing activated mitogen-activated protein kinases (MAPKs) access to
their nuclear targets; however, the mechanisms linking MAPK-induced
nuclear translocation and target gene expression mediating oncologic
activity remain obscure. Here, we show that the MAPK extracellular
signal-regulated kinase (ERK) 1, but not ERK2, phosphorylated
intestine-specific homeobox (ISX), leading to its nuclear translocation
and downstream oncogenic signaling. Mechanistically, ERK1 phosphorylated
serine 183 of ISX, facilitating its nuclear translocation and downstream
target gene expression. In contrast, dominant-negative ERK1 expression
in hepatoma cells inhibited the nuclear translocation of ISX and the
expression of downstream genes involved in cell proliferation, malignant
transformation, and epithelial-mesenchymal transition in vitro and in
vivo. An activating mutation in ISX (S183D) exhibited a constitutive
nuclear localization and resistance to sorafenib. Additionally, in 576
paired clinical hepatocellular carcinoma (HCC) samples and adjacent
normal tissues, ERK1 and ISX were co-expressed in a tumor-specific
manner at mRNA and protein levels, while their mRNA levels showed
significant correlation with survival duration, tumor size, number, and
stage. These results highlight the significance of ERK1/ISX signaling in
HCC progression and its potential as a prognostic and therapeutic target
in HCC.