Selective activation of the p38 MAPK pathway by synthetic monophosphoryl lipid A

J Biol Chem. 2009 Nov 13;284(46):31982-91. doi: 10.1074/jbc.M109.046383. Epub 2009 Sep 15.

Abstract

TLR4 stimulation by lipopolysaccharide can cause both MAL/MyD88- and TRAM/TRIF (Toll IL-1 receptor domain-containing adaptor-inducing IFNbeta)-dependent signaling events. Monophosphoryl lipid A (MPLA), a low toxicity derivative of endotoxic lipopolysaccharide, enhances antibody responses, T cell expansion, and recall responses against antigens without causing excessive inflammatory side effects. Previously, we proposed that TRIF-biased activation of TLR4 by MPLA is responsible for its reduced toxicity while retaining potent adjuvant effects. However, some TRIF-associated genes, such as MCP-1, are only weakly expressed, and some MyD88-associated inflammatory and anti-inflammatory cytokines, such as tumor necrosis factor alpha and interleukin-10, are strongly activated after MPLA stimulation despite weak NF-kappaB but strong IRF3 activation. We now report that synthetic derivatives of MPLA retained TRIF bias as compared with synthetic diphosphoryl lipid A, indicating a change in a single phosphoryl group is sufficient for TRIF-biased TLR4 stimulation. We extend our previous observations by showing that sMLA induces strong p38 MAPK but weak JNK activation, resulting in high IP-10 (interferon-inducible protein 10), tumor necrosis factor alpha, and interleukin-10 but low MCP-1 transcript levels. Results of this study identify a novel biochemical mechanism for regulation of sMLA-induced gene expression.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adaptor Proteins, Vesicular Transport / physiology*
  • Adjuvants, Immunologic / pharmacology*
  • Animals
  • Blotting, Western
  • Bone Marrow / metabolism
  • Chemokine CXCL10 / genetics
  • Chemokine CXCL10 / metabolism
  • Dendritic Cells / metabolism*
  • Lipid A / analogs & derivatives*
  • Lipid A / pharmacology
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Myeloid Differentiation Factor 88 / physiology*
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Reverse Transcriptase Polymerase Chain Reaction
  • Toll-Like Receptor 4 / genetics
  • Toll-Like Receptor 4 / metabolism
  • p38 Mitogen-Activated Protein Kinases / metabolism*

Substances

  • Adaptor Proteins, Vesicular Transport
  • Adjuvants, Immunologic
  • Chemokine CXCL10
  • Lipid A
  • Myd88 protein, mouse
  • Myeloid Differentiation Factor 88
  • RNA, Messenger
  • TICAM-1 protein, mouse
  • Tlr4 protein, mouse
  • Toll-Like Receptor 4
  • p38 Mitogen-Activated Protein Kinases
  • monophosphoryl lipid A