Toll-like Receptor (TLR)
Toll-like receptors (TLRs) are a class of proteins that play a key role in the innate immune system. They are single, membrane-spanning, non-catalytic receptors usually expressed in sentinel cells such as macrophages and dendritic cells, that recognize structurally conserved molecules derived from microbes. Once these microbes have breached physical barriers such as the skin or intestinal tract mucosa, they are recognized by TLRs, which activate immune cell responses. The TLRs include TLR1, TLR2, TLR3, TLR4, TLR5, TLR6, TLR7, TLR8, TLR9, TLR10, TLR11, TLR12, and TLR13. Toll-Like Receptors (TLRs) play a critical role in the early innate immune response to invading pathogens by sensing microorganism and are involved in sensing endogenous danger signals. TLRs are evolutionarily conserved receptors are homologues of the Drosophila Toll protein, discovered to be important for defense against microbial infection. TLRs recognize highly conserved structural motifs known as pathogen-associated microbial patterns (PAMPs), which are exclusively expressed by microbial pathogens.
||Motolimod is a selective Toll-like receptor (TLR) 8 agonist, with EC50 of about 100 nM.
||Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the levels of cytokines such as TNF-α, IL-6 and IFN-α.
||Gardiquimod trifluoroacetate is a specific TLR7 agonist which can also inhibit HIV-1 reverse transcriptase.
||Leonurine (hydrochloride), a major alkaloid compound extracted from Leonurus japonicas Houtt. (Labiatae), is considered to have antitumor roles.
||Atractylenolide I is a natural compound extracted from largehead atractylodes rhizome; induce apoptosis and bring about cytotoxicity of human promyeloleukemic HL-60 cells; TLR4-antagonizing agent.
||TLR7-agonist-1 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a LEC of 0.4 μM.
||E6446 dihydrochloride is a novel synthetic antagonist for nucleic acid-sensing TLRs; potently suppressed DNA stimulation of HEK:TLR9 cells with IC50 of 10 nM.
||CU-CPT-9b is a nolve TLR8 inhibitor.
||Semapimod (CNI 1493.
||IAXO-102 is a TLR4 antagonist, inhibits MAPK and p65 NF-kB phosphorylation involved in down regulation of the expression of TLR4 and TLR4 dependent proinflammatory protein. IAXO-102 prevents experimental abdominal aortic aneurysm development.
||Semapimod (CNI 1493.
||An orally available, small molecule TLR7/8/9 antagonist for the treatment of systemic lupus erythematosus and other autoimmune disorders..
||Gardiquimod is a TLR7 agonist, inducing the activation of NF-B in HEK293 cells expressing human or mouse TLR7.
||Gardiquimod hydrochloride is a TLR7 agonist, inducing the activation of NF-B in HEK293 cells expressing human or mouse TLR7.