Structure-based design of novel human Toll-like receptor 8 agonists.

@article{Kokatla2014StructurebasedDO,
  title={Structure-based design of novel human Toll-like receptor 8 agonists.},
  author={Hari Prasad Kokatla and Diptesh Sil and Hiromi Tanji and Umeharu Ohto and Subbalakshmi S. Malladi and Lauren M. Fox and Toshiyoki Shimizu and Sunil A David},
  journal={ChemMedChem},
  year={2014},
  volume={9 4},
  pages={719-23}
}
Toll-like receptor (TLR)-8 agonists activate adaptive immune responses by inducing robust production of T helper 1-polarizing cytokines, suggesting that TLR8-active compounds might be promising candidate vaccine adjuvants. Recently, a C2-butyl furo[2,3-c]quinoline was reported with purely TLR8 agonistic activity. This compound was successfully co-crystallized with the human TLR8 ectodomain, and the co-crystal structure revealed ligand-induced reorganization of the binding pocket of TLR8. The… CONTINUE READING
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