A Synthetic Lipid A Mimetic Modulates Human TLR4 Activity

Matteo Piazza, Valentina Calabrese, Gaetana Damore, Roberto Cighetti, Theresa L. Gioannini, Jerrold Weiss, Francesco Peri

ChemMedChem · 2011 · 18 citations · 31 references

Concepts

Abstract

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.

References

31