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Toll-like Receptors (TLR) Agonists - Ligands

The Toll-like receptors (TLRs) recognize pathogen-associated molecular patterns (PAMPs) to activate immunity and inflammatory cascades. The use of potent TLR ligands to activate, or TLR inhibitors to inhibit, TLR signaling cascades, enables the study of specific TLRs and their effect on the immune system.

  Ligand Description
TLR1 PAM3CSK4 A synthetic lipopeptide that mimics the acylated amino terminus of bacterial lipoproteins. It is recognized by a heterodimer that is formed between TLR1 and TLR2.
TLR2 PAM3CSK4 A synthetic lipopeptide that mimics the acylated amino terminus of bacterial lipoproteins. It is recognized by a heterodimer that is formed between TLR1 and TLR2.
MALP-2 A lipopeptide originally isolated from Mycoplasma fermentans. MALP-2 is recognized by a heterodimer formed between TLR2 and TLR6.
Zymosan A cell wall preparation of Saccharomyces cerevisiae and is composed primarily of glucans, mannans, mannoproteins and chitin. It activates TLR2 in synergistic collaboration with Dectin-1, a C-type lectin that is expressed on monocytes, macrophages, and dendritic cells as a phagocytic receptor for glucan containing particles
TLR3 Poly (I:C) A synthetic analog of double-stranded RNA, produced during the replication of many viruses; it binds directly to TLR3
TLR4 LPS A standard lipopolysaccharide preparation. LPS is a major component of the cell wall of Gram-negative bacteria. Recognition of LPS requires TLR4 in addition to CD14, and is enhanced by MD-2, a secreted glycoprotein which forms a receptor complex with TLR4.
TLR6 MALP-2 A lipopeptide originally isolated from Mycoplasma fermentans. MALP-2 is recognized by a heterodimer formed between TLR2 and TLR6.
TLR7 Imiquimod An imidazoquinoline amine analog to guanosine.
  Imidazoquinoline Resiquimod A synthetic imidazoquinoline. It has been demonstrated to activate TLR7 and TLR8.
TLR8 Imidazoquinoline Resiquimod A synthetic imidazoquinoline. It has been demonstrated to activate TLR7 and TLR8.
TLR9 CpG ODN Synthetic oligonucleotide containing unmethylated deoxycytosine-deoxyguanosine (CpG) motifs.

 

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