HLJ1 is an endogenous Src inhibitor suppressing cancer progression through dual mechanisms

Oncogene. 2016 Oct 27;35(43):5674-5685. doi: 10.1038/onc.2016.106. Epub 2016 Apr 11.

Abstract

HLJ1 (DNAJB4), a DNAJ/Hsp40 chaperone, has emerged as a novel prognostic marker in lung cancers; however, the molecular contribution and functionality in neoplastic diseases remain to be established. This study demonstrated that HLJ1 inhibits epithelial-mesenchymal transition in vitro and reduces lung cancer metastasis in vivo. Using shRNA silencing and ectopic expression of HLJ1, we found that HLJ1 not only suppresses catalytic activity of Src but also downregulates the formation of oncogenic complexes associated with the EGFR, FAK and STAT3 signaling pathways. A screen of specimens from HLJ1-knockout mice and lung cancer patients validated that HLJ1 expression is inversely correlated with Src activity. Mechanistically, HLJ1 protein directly bound to catalytic and protein-binding domains of Src through its amino acid Y172 and the P301/P304 motif. Following Src-induced HLJ1 phosphorylation at Y172, HLJ1-Src interaction was elevated, resulting in Src inhibition and malignancy suppression. Interestingly, both Src-binding regions also occurred in other DNAJB family members and contributed to anti-invasive activities of DNAJB proteins. We conclude that HLJ1 is an endogenous Src inhibitor that can suppress cancer metastasis through complex interacting mechanisms. This HLJ1-Src complex might provide a promising molecular model for developing new anticancer strategies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Disease Models, Animal
  • Disease Progression
  • Enzyme Activation
  • Gene Expression
  • Gene Expression Regulation, Neoplastic
  • Gene Knockdown Techniques
  • HSP40 Heat-Shock Proteins / chemistry
  • HSP40 Heat-Shock Proteins / genetics
  • HSP40 Heat-Shock Proteins / metabolism*
  • HSP40 Heat-Shock Proteins / pharmacology
  • Humans
  • Lung Neoplasms / genetics
  • Lung Neoplasms / metabolism
  • Lung Neoplasms / pathology
  • Male
  • Mice
  • Mice, Knockout
  • Models, Biological
  • Models, Molecular
  • Mutation
  • Neoplasm Invasiveness
  • Neoplasm Metastasis
  • Neoplasms / genetics
  • Neoplasms / metabolism*
  • Neoplasms / pathology*
  • Protein Binding
  • Protein Conformation
  • Protein Interaction Domains and Motifs
  • RNA Interference
  • RNA, Small Interfering / genetics
  • src Homology Domains
  • src-Family Kinases / antagonists & inhibitors*
  • src-Family Kinases / chemistry
  • src-Family Kinases / metabolism

Substances

  • DNAJB4 protein, human
  • HSP40 Heat-Shock Proteins
  • RNA, Small Interfering
  • src-Family Kinases