Table 2.
TLR4 antagonists presented in this review, ranked by chemical structure (glycolipid or non-glycolipid), stage of drug development, and mechanism of action (MOA).
| Compound | Class | Drug Development Stage | MOA |
|---|---|---|---|
| FP7-like (35, 36) | Glycolipid based | In vivo | Competitive inhibition |
| LAM (37) | Glycolipid based | In vitro | Competitive inhibition |
| IAXO (38) | Glycolipid based | In vivo | Competitive inhibition; LPS sequestration |
| TAK-242 (39) | Non-glycolipid | Clinical | Non-competitive inhibition |
| Calixarenes (40) | Non-glycolipid | In vitro | Competitive inhibition |
| Opioid (41) | Non-glycolipid | In vitro | Competitive inhibition |
| Pip2 (42) | Non-glycolipid | In vivo | Competitive inhibition |
| Unsaturated cardiolipins (33) | Non-glycolipid | In vitro | Competitive inhibition |
| Alpinetin (43) | Non-glycolipid | In vivo | Down-regulation of TLR4 expression |
| Ferulic acid (44) | Non-glycolipid | In vivo | TLR4/MD-2 complex disruption |