RAC1-GTP promotes epithelial-mesenchymal transition and invasion of colorectal cancer by activation of STAT3

Lab Invest. 2018 Aug;98(8):989-998. doi: 10.1038/s41374-018-0071-2. Epub 2018 Jun 8.

Abstract

Epithelial-mesenchymal transition (EMT) plays a critical role in initiating tumor invasion and metastasis of colorectal cancer (CRC), although the underlying mechanisms remain to be clarified. Herein, we demonstrate that the active form of Rac family small GTPase 1 (RAC1-GTP) is overexpressed in CRCs and promotes the EMT-mediated invasion of CRC cells through activation of the signal transducers and activators of transcription 3 (STAT3) pathway. Increased expression of RAC1-GTP in CRC tissues was positively correlated with the TNM stages of CRCs and indicated poor prognosis of CRC patients. Targeting RAC1-GTP activity by its specific inhibitor NSC23766 markedly suppressed the migration and invasion of CRC cells. Mechanistically, RAC1-GTP directly interacted with STAT3 to promote STAT3 phosphorylation, thus promoted EMT of CRC cells. Enforced expression of constitutively activated STAT3 (STAT3-C) abrogated the suppressive effect of RAC1-GTP disruption on the migration and invasion of CRC cells. Importantly, NSC23766 disrupted EMT in CRC cells and significantly diminished growth of CRC xenografts. Taken together, our data indicate that RAC1-GTP is an important player in EMT-mediated tumor invasion and a potential therapeutic target for CRCs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminoquinolines / pharmacology
  • Animals
  • Cell Line, Tumor
  • Cell Movement / drug effects
  • Colorectal Neoplasms / metabolism*
  • Colorectal Neoplasms / pathology
  • Epithelial-Mesenchymal Transition*
  • Female
  • HCT116 Cells
  • Humans
  • Male
  • Mice, Nude
  • Middle Aged
  • Neoplasm Invasiveness
  • Phosphorylation
  • Protein Binding
  • Pyrimidines / pharmacology
  • STAT3 Transcription Factor / metabolism*
  • Tumor Burden / drug effects
  • Xenograft Model Antitumor Assays / methods
  • rac1 GTP-Binding Protein / antagonists & inhibitors
  • rac1 GTP-Binding Protein / metabolism*

Substances

  • Aminoquinolines
  • NSC 23766
  • Pyrimidines
  • STAT3 Transcription Factor
  • rac1 GTP-Binding Protein