Syntheses of human TLR8-specific small-molecule agonists

Mallesh Beesu, Hari Prasad Kokatla, Sunil A. David

Research output: Chapter in Book/Report/Conference proceedingChapter

4 Scopus citations


Human toll-like receptor (hTLR)-8 is expressed in myeloid dendritic cells, monocytes, and monocytederived dendritic cells. Engagement by TLR8 agonists evokes a distinct cytokine profile which favors the development of type 1 helper T cells. Focused exploration of structure-activity relationships in the imidazoquinolines has led to the identification of several novel human TLR8-specific agonists. The synthetic procedures for best-in-class analogues encompassing four chemotypes are described.

Original languageEnglish (US)
Title of host publicationMethods in Molecular Biology
PublisherHumana Press Inc.
Number of pages16
StatePublished - 2017

Publication series

NameMethods in Molecular Biology
ISSN (Print)1064-3745

Bibliographical note

Funding Information:
This work was supported by NIH/NIAID contracts HSN272200900033C and HHSN272201400056C.

Publisher Copyright:
© Springer Science+Business Media New York 2017.


  • Innate immunity
  • TLR8
  • TLR8 agonists
  • Vaccine adjuvants


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