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A Synthetic Lipid A Mimetic Modulates Human TLR4 Activity
Author(s) -
Piazza Matteo,
Calabrese Valentina,
Damore Gaetana,
Cighetti Roberto,
Gioannini Theresa,
Weiss Jerrold,
Peri Francesco
Publication year - 2012
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201100494
Subject(s) - tlr4 , chemistry , agonist , receptor , lipid a , biochemistry , vaccine adjuvant , pharmacology , adjuvant , biology , immunology , lipopolysaccharide
The sincerest form of flattery! A novel, symmetric lipid A mimetic (D1) formed by two glucose units linked through a 6‐6' succinic diamide linker is active in modulating the activity of human TLR4. D1 inhibits endotoxin‐stimulated TLR4 activation by inhibiting interaction of endotoxin with both receptors CD14 and MD‐2 (associated to TLR4). D1 also has weak TLR4 agonist activity that makes it a promising lead compound for development as a vaccine adjuvant.