Scientific article
Open access

Toll-like receptor activation of human cells by synthetic triacylated lipid A-like molecules

Published inThe Journal of biological chemistry, vol. 287, no. 20, p. 16121-16131
Publication date2012

Recognition of microbial molecules by mammalian host receptors is essential to mount an immune response. Hexaacylated LPS is the prototypic example of a bacterial molecule recognized by the receptor complex TLR4/MD-2 with its lipid A moiety, whereas bacterial lipopeptides are recognized by TLR2. Here we show that a series of synthetic triacylated lipid A-like molecules are weak Toll-like receptor (TLR) agonists (mainly TLR2 agonists) but very potent TLR4/MD-2 antagonists (submicromolar range). Not only do they block human cell responses to LPS but also to whole gram-negative bacteria, and they inhibit the phagocytosis of gram-negative bacteria. These compounds may represent promising immunomodulatory agents.

  • Gram-Negative Bacteria/immunology/metabolism
  • HEK293 Cells
  • Humans
  • Immunologic Factors/chemical synthesis/immunology/pharmacology
  • Lipid A/chemical synthesis/immunology/pharmacology
  • Lymphocyte Antigen 96/immunology/metabolism
  • Toll-Like Receptor 2/agonists/antagonists & inhibitors/immunology/metabolism
  • Toll-Like Receptor 4/agonists/antagonists & inhibitors/immunology/metabolism
Citation (ISO format)
DUNN-SIEGRIST, Irène et al. Toll-like receptor activation of human cells by synthetic triacylated lipid A-like molecules. In: The Journal of biological chemistry, 2012, vol. 287, n° 20, p. 16121–16131. doi: 10.1074/jbc.M112.348383
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Article (Published version)
ISSN of the journal0021-9258

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