An inhibitor we would use to target TLR3 is (R)-2-(3-chloro-6-fluorobenzo[b]thiophene-2-carboxamido)-3-phenylpropanoic acid (4a) a compound known as 4a. It is an antagonist to TLR3 signaling and is also known to inhibit the expression of downstream signaling pathways assisted by the TLR3/dsRNA complex. This compound is able to inhibit TLR3 signaling and does not affect other types of TLRs which illustrates its highly selectivity characteristic. It also holds the property of being low cytotoxicity. In order to further emphasize that it directly binds to TLR3, a fluorescence anisotropy assay demonstrated that it competes with dsRNA, which we know is involved in activating TLRs.
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