Selective targeting of the TLR4 co-receptor, MD2, prevents colon cancer growth and lung metastasis

Int J Biol Sci. 2020 Feb 17;16(8):1288-1302. doi: 10.7150/ijbs.39098. eCollection 2020.

Abstract

Toll-like receptor (TLR) signaling is an emerging pathway in tumor cell invasion and metastasis. Myeloid differentiation protein-2 (MD2) contributes to ligand recognition and activation of TLRs in response to exogenous microbial insults or endogenous agents. We hypothesized that blocking MD2 using a specific inhibitor would prevent TLR4-mediated inflammatory responses and metastatic cancer growth. Here, we report that a MD2 inhibitor, L6H21, inhibited migration and invasion of LPS-activated colon cancer CT26.WT cells. These activities were accompanied by inhibition of nuclear factor-κB (NF-κB) activation, and thereby inhibition of the production of pro-inflammatory cytokines and adhesive molecules in colon cancer cells. Furthermore, L6H21 inhibited CT26.WT metastasis to the lung in BALB/c mice as well as suppressed colitis-induced colon cancer induced by azoxymethane/dextran sulfate sodium (AOM/DSS). Taken together, our results demonstrated that L6H21 suppressed tumor invasion and metastasis through blocking TLR4-MD2/NF-κB signaling axis. These findings reveal that inhibition of MD2 may be an important target for the development of colon cancer therapies.

Keywords: MD2; NF-κB; TLR4; colitis-induced colon cancer; colon cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Blotting, Western
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Chalcones / pharmacology
  • Colonic Neoplasms / complications*
  • Colonic Neoplasms / drug therapy
  • Colonic Neoplasms / metabolism*
  • Enzyme-Linked Immunosorbent Assay
  • Gene Silencing
  • Humans
  • Immunoprecipitation
  • Lung Neoplasms / metabolism*
  • Lung Neoplasms / prevention & control
  • Lung Neoplasms / secondary*
  • Lymphocyte Antigen 96 / antagonists & inhibitors*
  • Lymphocyte Antigen 96 / metabolism*
  • Male
  • Middle Aged
  • Neoplasm Metastasis / prevention & control
  • Real-Time Polymerase Chain Reaction
  • Signal Transduction / drug effects
  • Toll-Like Receptor 4 / metabolism*

Substances

  • 2,3-dimethoxy-4'-ethoxychalcone
  • Chalcones
  • LY96 protein, human
  • Lymphocyte Antigen 96
  • Toll-Like Receptor 4