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. 2023 Aug 7;44(12):2358–2375. doi: 10.1038/s41401-023-01123-5

Table 2.

Drugs for AS associated with TLR signaling pathways.

Drugs Effect on TLR signaling pathways Mechanism of actions References
Atorvastatin Inhibits TLR4 Reduces levels of miRNA-146a/b, IRAK1 mRNA, TRAF6 mRNA, and TLR4 mRNA Kong et al. [195]
Simvastatin Inhibits TLR2 and TLR4 Reduces TLR4 and TLR2 membrane expression on monocytes and cytokine production (IL-6 and IL-1β). Koike et al. [196]
Fluvastatin Inhibits TLR2 and TLR4 Reduces TLR expression and limits this process dramatically Kapelouzou et al. [168]
7-Deacetyl-gedunin Inhibits LPS/TLR4 signaling Inhibits expression of pro-inflammatory mediators (iNOS, TNF-α, IL- 1β) Chen et al. [197]
Phenethyl Inhibits TLR3 signaling Reduces LPS-induced inflammation and downregulates pro-inflammatory protein expression (TNF-α, IL-6, COX-2, iNOS). Cong et al. [111]
Resiquimod Activates TLR7 signaling [184] Attenuates pulmonary inflammation Nadeem et al. [198]
Sulforaphane Inhibits TLR3-mediated NF-κB signaling Neutralizes neuroinflammation (regulates NO, IL-1β, IL-6, and TNF-α and inhibits phosporylation of MAPKs) Mohan et al. [199]
CQ, HCQ Block TLR7/8/9 Relieve endothelial dysfunction Gomez-Guzman et al. [200]
SMU-CX24 Inhibits TLR3 Suppression of TLR3 expression and decrease in inflammatory infiltration in atherosclerotic lesions Chen et al. [147]
Valsartan Blocks TLR4 Reduces the release of proinflammatory cytokines and infarct size El-Salamouni et al. [201]
Candesartan Inhibits TLR2/4 Suppresses Pam3CSK4 and LPS induced TLR2 and TLR4 activation Atwa et al. [202]
T2.5 Inhibits TLR2 Inhibits the recruitment and inflammation of macrophages in the heart Wang et al. [158]
NI-0101 Inhibits TLR4 Inhibits TLR4 signaling by blocking TLR4 dimerization Monnet et al. [161]
miR-146a Inhibits TLR4 Impedes the translation of TRAF6 and IRAK1, which are both located downstream of the TLR4 signal. Pan et al. [152]
HDL-like NP Inhibits TLR4 Inhibits LPS induced NF-κB signaling Foit et al. [155]
Peptide-GNP hybrid Inhibits TLR2/3/4/5 Inhibits both NF-κB and IRF pathways Yang et al. [156]
P12 Inhibits TLR2, TLR3, TLR4 and TLR5 Corrects LPS-induced gene expressions, reduces future pro-inflammatory cytokine production (IL-12p40, MCP-1, and IFN-γ), and elevates the anti-inflammatory cytokine IL-1RA Gao et al. [143]
alirocumab Inhibits PCSK9 Reduces endothelial expression of ICAM-1 and Ly6Chi monocytes Hoogeveen et al. [169]
canakinumab anti-IL-1β Reduces LPS-induced endothelium activation in vitro by inhibiting NF-κB transcriptional activity. Ridker et al. [175]