Abstract: A peptide inhibiting a Toll-like receptor (TLR) signaling pathway is disclosed. The peptide strongly binds to a TIR-containing molecule to inhibit the TLR, in particular, the TLR4 signaling pathway. A fusion peptide in which a cell-penetrating peptide is conjugated to said peptide; a TLR4 antagonist comprising said peptide or said fusion peptide; and compositions and methods for preventing or treating autoimmune diseases or inflammatory diseases are disclosed. The peptide exhibits an inhibitory effect on a wide range of TLR signaling pathways including TLR4, blocks MyD88- and TRIF-dependent TLR4 pathways, and has a substantial disease-alleviating effect in mouse models of rheumatoid arthritis, psoriasis, systemic lupus erythematosus, and non-alcoholic steatohepatitis, and thus can be usefully utilized as therapeutics for immune-related diseases and inflammatory diseases that require negative control of TLR.

Abstract: The present disclosure relates to a novel small molecule TLR2 antagonist, and particularly, to 19 novel TLR2 antagonists, a pharmaceutical composition, including the antagonists, for preventing or treating inflammatory diseases, and a TLR4 regulator. The novel TLR2 antagonists according to the present disclosure can be effectively used as a preparation for oral administration by having low molecular weight and high oral bioavailability, and can be useful in pharmaceutical compositions for preventing or treating inflammatory diseases since the secretion of IL-8 is effectively inhibited and in vivo cytotoxicity is not induced. In addition, the novel TLR2 antagonists according to the present disclosure can be used as a TLR4 regulator.

Abstract: The present disclosure relates to a novel small molecule TLR2 antagonist, and particularly, to 19 novel TLR2 antagonists, a pharmaceutical composition, including the antagonists, for preventing or treating inflammatory diseases, and a TLR4 regulator. The novel TLR2 antagonists according to the present disclosure can be effectively used as a preparation for oral administration by having low molecular weight and high oral bioavailability, and can be useful in pharmaceutical compositions for preventing or treating inflammatory diseases since the secretion of IL-8 is effectively inhibited and in vivo cytotoxicity is not induced. In addition, the novel TLR2 antagonists according to the present disclosure can be used as a TLR4 regulator.