Incorporation of Phosphonate into Benzonaphthyridine Toll-like Receptor 7 Agonists for Adsorption to Aluminum Hydroxide.

@article{Cortz2016IncorporationOP,
  title={Incorporation of Phosphonate into Benzonaphthyridine Toll-like Receptor 7 Agonists for Adsorption to Aluminum Hydroxide.},
  author={Alex Orellana Cort{\'e}z and Yongkai Li and Andrew Todd Miller and Xiaoyue Zhang and Kathy Yue and Jillian Maginnis and Janice Hampton and De Shon Hall and Michael Jeremy Shapiro and Bishnu Nayak and Ugo D'Oro and Chun Xing Li and David A. G. Skibinski and Moustapha Mbow and Manmohan Singh and Derek T O'hagan and Michael Peter Cooke and Nicholas M. Valiante and Tom Y-H Wu},
  journal={Journal of medicinal chemistry},
  year={2016},
  volume={59 12},
  pages={
          5868-78
        }
}
Small molecule Toll-like receptor 7 (TLR7) agonists have been used as vaccine adjuvants by enhancing innate immune activation to afford better adaptive response. Localized TLR7 agonists without systemic exposure can afford good adjuvanticity, suggesting peripheral innate activation (non-antigen-specific) is not required for immune priming. To enhance colocalization of antigen and adjuvant, benzonaphthyridine (BZN) TLR7 agonists are chemically modified with phosphonates to allow adsorption onto… CONTINUE READING

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