tlr5

TH1020 is a novel Inhibitor of Toll-Like Receptor 5 (TLR5)/Flagellin Complex with promising activity (IC50 =0.85±0.12 μm) and specificity.

EGFRvIII peptide, a synthetic peptide mirroring the EGFRvIII fusion junction—a tumor-specific, perpetually active EGFR variant missing amino acids 6-273 of the wild-type—binds to HLA-A*0201-positive T2 cells under MHC class I at 25 µg/ml. It enables antigen presentation in dendritic cells from human peripheral blood mononuclear cells (PBMCs), thus activating CD8+ cytotoxic T lymphocytes and prompting IFN-γ production. Administered at 15 µg/animal with the TLR5 agonist flagellin B, EGFRvIII peptide elevates CD8+ T cell numbers, lowers regulatory T cells (Tregs) in the brain, diminishes tumor volume, and extends survival in a GL261 glioblastoma mouse model.

Flagellin from S. typhimurium is an effective TLR5 agonist. It can activate immune cells and inhibit the activity of melanoma cells.

Entolimod (CBLB-502) is a recombinant protein that serves as an agonist for Toll-like receptor 5 (TLR5). It triggers the TLR5-NF-κB signaling cascade, leading to the mobilization of various components of both innate and adaptive immunity to the liver, subsequently inhibiting liver metastases and establishing long-term antitumor immune memory.