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Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo.
Lamphier M, Zheng W, Latz E, Spyvee M, Hansen H, Rose J, Genest M, Yang H, Shaffer C, Zhao Y, Shen Y, Liu C, Liu D, Mempel TR, Rowbottom C, Chow J, Twine NC, Yu M, Gusovsky F, Ishizaka ST. Lamphier M, et al. Mol Pharmacol. 2014 Mar;85(3):429-40. doi: 10.1124/mol.113.089821. Epub 2013 Dec 16. Mol Pharmacol. 2014. PMID: 24342772
Binding of the compounds to DNA prevents DNA-TLR9 interaction in vitro and modulates signaling in vivo. Our data also confirm an earlier report that this same mechanism may explain inhibition of TLR7 and 9 signaling by hydroxychloroquine (Plaquenil; Sa …
Binding of the compounds to DNA prevents DNA-TLR9 interaction in vitro and modulates signaling in vivo. Our data also confirm an earl …
Hydroxychloroquine Inhibits Macrophage Activation and Attenuates Renal Fibrosis After Ischemia-Reperfusion Injury.
Zheng H, Zhang Y, He J, Yang Z, Zhang R, Li L, Luo Z, Ye Y, Sun Q. Zheng H, et al. Front Immunol. 2021 Apr 14;12:645100. doi: 10.3389/fimmu.2021.645100. eCollection 2021. Front Immunol. 2021. PMID: 33936063 Free PMC article.
Chronic kidney disease (CKD), which is associated with high morbidity, remains a worldwide health concern, while effective therapies remain limited. Hydroxychloroquine (HCQ), which mainly targets toll-like receptor-7 (TLR-7) and TLR-9, is associated with a lower risk of in …
Chronic kidney disease (CKD), which is associated with high morbidity, remains a worldwide health concern, while effective therapies remain …
Mechanism of endosomal TLR inhibition by antimalarial drugs and imidazoquinolines.
Kuznik A, Bencina M, Svajger U, Jeras M, Rozman B, Jerala R. Kuznik A, et al. J Immunol. 2011 Apr 15;186(8):4794-804. doi: 10.4049/jimmunol.1000702. Epub 2011 Mar 11. J Immunol. 2011. PMID: 21398612
In the therapy of systemic lupus erythematosus, antimalarial drugs chloroquine, hydroxychloroquine, and quinacrine have been used for a long time. Their suppression of endosomal TLR activation has been attributed to the inhibition of endosomal acidification, which is a pre …
In the therapy of systemic lupus erythematosus, antimalarial drugs chloroquine, hydroxychloroquine, and quinacrine have been used for …