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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

E5531, a pure endotoxin antagonist of high potency.

Shock due to Gram-negative bacterial sepsis is a consequence of acute inflammatory response to lipopolysaccharide (LPS) or endotoxin released from bacteria. LPS is a major constituent of the outer membrane of Gram-negative bacteria, and its terminal disaccharide phospholipid (lipid A) portion contains the key structural features responsible for toxic activity. Based on the proposed structure of nontoxic Rhodobacter capsulatus lipid A, a fully stabilized endotoxin antagonist E5531 has been synthesized. In vitro, E5531 demonstrated potent antagonism of LPS-mediated cellular activation in a variety of systems. In vivo, E5531 protected mice from LPS-induced lethality and, in cooperation with an antibiotic, protected mice from a lethal infection of viable Escherichia coli.[1]


  1. E5531, a pure endotoxin antagonist of high potency. Christ, W.J., Asano, O., Robidoux, A.L., Perez, M., Wang, Y., Dubuc, G.R., Gavin, W.E., Hawkins, L.D., McGuinness, P.D., Mullarkey, M.A. Science (1995) [Pubmed]
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