Met/Hepatocyte growth factor receptor ubiquitination suppresses transformation and is required for Hrs phosphorylation

JV Abella, P Peschard, MA Naujokas, T Lin… - … and cellular biology, 2005 - Taylor & Francis
JV Abella, P Peschard, MA Naujokas, T Lin, C Saucier, S Urbé, M Park
Molecular and cellular biology, 2005Taylor & Francis
The Met receptor tyrosine kinase (RTK) regulates epithelial remodeling, dispersal, and
invasion and is deregulated in many human cancers. It is now accepted that impaired down-
regulation, as well as sustained activation, of RTKs could contribute to their deregulation.
Down-regulation of the Met receptor involves ligand-induced internalization, ubiquitination
by Cbl ubiquitin ligases, and lysosomal degradation. Here we report that a ubiquitination-
deficient Met receptor mutant (Y1003F) is tumorigenic in vivo. The Met Y1003F mutant is …
The Met receptor tyrosine kinase (RTK) regulates epithelial remodeling, dispersal, and invasion and is deregulated in many human cancers. It is now accepted that impaired down-regulation, as well as sustained activation, of RTKs could contribute to their deregulation. Down-regulation of the Met receptor involves ligand-induced internalization, ubiquitination by Cbl ubiquitin ligases, and lysosomal degradation. Here we report that a ubiquitination-deficient Met receptor mutant (Y1003F) is tumorigenic in vivo. The Met Y1003F mutant is internalized, and undergoes endosomal trafficking with kinetics similar to the wild-type Met receptor, yet is inefficiently targeted for degradation. This results in sustained activation of Met Y1003F and downstream signals involving the Ras-mitogen-activated protein kinase pathway, cell transformation, and tumorigenesis. Although Met Y1003F undergoes endosomal trafficking and localizes with the cargo-sorting protein Hrs, it is unable to induce phosphorylation of Hrs. Fusion of monoubiquitin to Met Y1003F is sufficient to decrease Met receptor stability and prevent sustained MEK1/2 activation. In addition, this rescues Hrs tyrosine phosphorylation and decreases transformation in a focus-forming assay. These results demonstrate that Cbl-dependent ubiquitination is dispensable for Met internalization but is critical to target the Met receptor to components of the lysosomal sorting machinery and to suppress its inherent transforming activity.
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