Inhibition of the deubiquitinase USP5 leads to c-Maf protein degradation and myeloma cell apoptosis

Cell Death Dis. 2017 Sep 21;8(9):e3058. doi: 10.1038/cddis.2017.450.

Abstract

The deubiquitinase USP5 stabilizes c-Maf, a key transcription factor in multiple myeloma (MM), but the mechanisms and significance are unclear. In the present study, USP5 was found to interact with c-Maf and prevented it from degradation by decreasing its polyubiquitination level. Specifically, the 308th and 347th lysine residues in c-Maf were critical for USP5-mediated deubiquitination and stability. There are five key domains in the USP5 protein and subsequent studies revealed that the cryptic ZnF domain and the C-box domain interacted with c-Maf but the UBA1/UBA2 domain partly increased its stability. Notably, MafA and MafB are also members of the c-Maf family, however, USP5 failed to deubiquitinate MafA, suggesting its substrate specificity. In the functional studies, USP5 was found to promoted the transcriptional activity of c-Maf. Consistent with the high level of c-Maf protein in MM cells, USP5 was also highly expressed. When USP5 was knocked down, c-Maf underwent degradation. Interestingly, USP5 silence led to apoptosis of MM cells expressing c-Maf but not MM cells lacking c-Maf, indicating c-Maf is a key factor in USP5-mediated MM cell proliferation and survival. Consistent with this finding, WP1130, an inhibitor of several Dubs including USP5, suppressed the transcriptional activity of c-Maf and induced MM cell apoptosis. When c-Maf was overexpressed, WP1130-induced MM cell apoptosis was abolished. Taken together, these findings suggest that USP5 regulates c-Maf stability and MM cell survival. Targeting the USP5/c-Maf axis could be a potential strategy for MM treatment.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis* / genetics
  • Endopeptidases / chemistry
  • Endopeptidases / metabolism*
  • Gene Knockdown Techniques
  • HEK293 Cells
  • Humans
  • Lysine / metabolism
  • Molecular Targeted Therapy
  • Multiple Myeloma / genetics
  • Multiple Myeloma / metabolism*
  • Multiple Myeloma / pathology*
  • Polyubiquitin / metabolism
  • Protein Binding
  • Protein Domains
  • Protein Stability
  • Proteolysis*
  • Proto-Oncogene Proteins c-maf / metabolism*
  • Structure-Activity Relationship
  • Transcription, Genetic
  • Ubiquitination

Substances

  • Proto-Oncogene Proteins c-maf
  • Polyubiquitin
  • Endopeptidases
  • ubiquitin isopeptidase
  • Lysine