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. 2017 Oct 21;174(Suppl Suppl 1):S225–S271. doi: 10.1111/bph.13876
Nomenclature TLR1 TLR2 TLR3 TLR4 TLR5
HGNC, UniProt TLR1, Q15399 TLR2, O60603 TLR3, O15455 TLR4, O00206 TLR5, O60602
Agonists compound 13 [91], peptidoglycan [163, 205] poly(I:C) [5] LPS [150], paclitaxel [85] – Mouse flagellin [67]
Selective antagonists resatorvid [78]
Comments Functions as a heterodimer with TLR2 in detection of triacylated lipoproteins. Activated by the synthetic analogue Pam3CSK4. Functions as a heterodimer with either TLR1 or TLR6 in the detection of triacylated and diacylated lipopeptides respectively. TLR1/2 and 2/6 heterodimers can be activated by the synthetic lipopeptides Pam3CSK4 and Pam2CSK4 respectively. There is some debate in the field as to whether or not peptidoglycan is a direct agonist of TLR2, or whether the early studies reporting this contained contaminating lipoproteins. Involved in endosomal detection of dsRNA; pro‐inflammatory. eritoran (E5564) is a lipid A analogue, which has been described as a TLR4 antagonist [79]. TLR4 signals in conjunction with the co‐factor MD‐2 (LY96). Involved in the detection of bacterial flagellin; pro‐inflammatory.