Selective TIR domain-targeting toll-like receptor 2 (TLR2) antagonist that inhibits human TLR2/1- & TLR2/6-, murine TLR2/1-, but not murine TLR2/6-mediated signaling.
TLR2-IN-C29 is a toll/IL-1 receptor resistance (TIR) domain BB loop-targeting, selective toll-like receptor 2 (TLR2) antagonist that inhibits both human TLR2/1 and TLR2/6-mediated signaling (IC50 = 37.6/19.7 μM against 50 ng/mL Pam3CSK/Pam2CSK-induced reporter signal, respectively, using HEK293T TLR2/6 or TLR2/1 transfectants), while blocking only murine TLR2/1-, but not murine TLR2/6-, mediated signaling (1h 25-50 μM C29 treatment prior to 50 ng P3C/mL or 100 ng P2C/mL for 1h in murine macrophages), nor signaling induced by other TLR agonists and TNF-α.
Frontiers in pharmacology, 13, 838873-838873 (2022-04-05)
Tetrastigma hemsleyanum Diels et Gilg (Sanyeqing, SYQ) has traditionally been used to treat inflammation, high fever and improve immune function of patients. Polysaccharides have been proved to be one of the important components of SYQ. Previous studies have confirmed the
Toll-like receptor 2 (TLR2) forms heterodimers with either TLR1 or TLR6 to induce protective early inflammatory responses to pathogen- and damage-associated molecular patterns. However, excessive activation is associated with inflammatory and metabolic diseases. Several TLR2 antagonists have been described but
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