TABLE 2

TLR ligands and clinically relevant TLR modulators

TLRExogenous and Endogenous LigandsTLR Modulators under Clinical Developmenta
AgonistsAntagonists
TLR1Bacterial lipopeptides
TLR2Bacterial lipoproteins and glycolipidsOPN-305 (antibody; inflammation, autoimmunity, ischemia/reperfusion, preclinical)
Endogenous HMGB1, HSP70, EDN, HA, HS
TLR2/TLR1Bacterial diacyl lipopeptides
TLR2/TLR6Bacterial triacyl lipopeptides
TLR3Viral double-stranded RNAAMP-516 (rintatolimod; viral infections, phase II)
Poly I:C (vaccine adjuvants, phase III)
TLR4Bacterial LPSPollinex Quattro (allergy, phase III)NI-0101 (antibody; acute and chronic inflammation, preclinical)
Endogenous HMGB1, HSP60, HSP70, EDN, HA, HS, Fibrinogen, S100 protein
TLR5Bacterial flagellinVax102, flagellin.HuHA, and flagellin.AvHA fusion proteins (vaccine adjuvants: bacterial, viral infections, phase I)
TLR6Bacterial triacyl lipopeptides
Fungal zymosan
TLR7Viral single-stranded RNAAZD8848 (asthma and allergic rhinitis, phase IIa)b
R-848 (resiquimod) (infectious diseases, phase II)
TLR8Viral single-stranded RNAR-848 (resiquimod) (infectious diseases, phase II)
TLR9Bacterial and viral CpG-DNAISS1018 (adjuvant allergy, phase II)c
AVE675 (asthma and allergic rhinitis, phase I)d
IMO-2134 (allergy, asthma, phase I)e
SAR-21609 (asthma)d
TLR10Unknown
TLR11Profilin

  • EDN, eosinophil-derived neurotoxin; HA, hyaluronan; HS, heparan sulfate.

  • ↵a Data from from Basith et al. (2011).

  • ↵b Ikeda et al. (2010).

  • ↵c Friedberg et al. (2009).

  • ↵e Heijink and Van Oosterhout (2006); Parkinson (2008).

  • ↵e Kline and Krieg (2008).