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Toll-like Receptor (TLR) Inhibitors

Both extracellular and intracellular pattern-associated molecular patterns (PAMPs) bind to Toll-like receptors (TLR) and activate downstream TLR signaling pathways via the interaction of TIR domains with adaptor molecules. This leads to NF-kB pathway activation, which in turn induces inflammatory responses. The TLRs and their downstream signaling pathways can be studied with cell-permeable inhibitor peptides. Inhibitor peptides block signaling events through decoy action: a realistic replica used as a lure or bait. Each peptide employs a specific decoy mechanism that blocks the propagation of downstream signaling pathways.

Target Inhibitor Description
TLR2 TIRAP Inhibitor Functions as a TIRAP decoy by binding TIR interacting domains on certain TLR receptors. Inhibits TIRAP-TLR2 and TIRAP-TLR4.
TLR4             

TIRAP Inhibitor

            

VIPER Inhibitor

            
            

Functions as a TIRAP decoy by binding TIR interacting domains on certain TLR receptors. Inhibits TIRAP-TLR2 and TIRAP-TLR4.

            

Binds TIRAP-TLR4 and TRAM-TLR4, inhibiting TLR4 activation.

            
MyD88 MyD88 Inhibitor Functions as a decoy by binding the MyD88 TIR domain.
IKK-gamma IKK-gamma Inhibitor Functions as a IKK-alpha and IKK-beta decoy by binding to IKK-gamma, preventing formation of the IKK complex.
NfKB p65 (pSer276) NfKB p65 Inhibitor Functions as a p65 decoy through phosphorylation of Ser276 on the peptide.
NfKB p65 (pSer529/536) NfKB p65 Inhibitor Functions as a p65 decoy through phosphorylation of Ser529/536 on the peptide.
NfKB p105/p50 (pSer105/p50) NfKB p50 Inhibitor Functions as a p65 decoy by blocking the intracellular recognition mechanism of p50 NLS.
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