C-ter TLR7 dimer binds HCQ

Stable Identifier
Reaction [binding]
Homo sapiens
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Toll-like receptor 7 (TLR7) is a key component of innate and adaptive immunity. It controls the host immune response against pathogens by stimulating dendritic cells and macrophages to secrete interferon alpha and other proinflammatory and regulatory cytokines (Lenert 2010). Hydroxychloroquine (HCQ) binds and antagonises TLR7 (Lamphier et al. 2014), and thus inhibits interferon alpha production. HCQ is used clinically to treat systemic lupus erythromatosis and other autoimmune disorders (Costedoat Chalumeau et al. 2014).

HCQ’s immunomodulatory properties may be useful for treatment of patients with COVID-19 (Sinha & Balayla 2020, Colson et al. 2020).
Literature References
PubMed ID Title Journal Year
31283223 Novel and Selective TLR7 Antagonists among the Imidazo[1,2-a]pyrazines, Imidazo[1,5-a]quinoxalines, and Pyrazolo[1,5-a]quinoxalines Series

Bou Karroum, N, Cuq, P, Moarbess, G, Bouharoun-Tayoun, H, Guichou, JF, Diab-Assaf, M, Bonnet, PA, Deleuze-Masquefa, C, Chamat, S, Kassab, I, Patinote, C

J. Med. Chem. 2019
24855048 Hydroxychloroquine: a multifaceted treatment in lupus

Le Guern, V, Morel, N, Guettrot-Imbert, G, Dunogué, B, Costedoat-Chalumeau, N

Presse Med 2014
24342772 Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo

Chow, J, Shaffer, C, Zhao, Y, Shen, Y, Mempel, TR, Spyvee, M, Zheng, W, Latz, E, Yang, H, Rose, J, Lamphier, M, Yu, M, Genest, M, Liu, C, Ishizaka, ST, Twine, NC, Liu, D, Hansen, H, Gusovsky, F, Rowbottom, C

Mol. Pharmacol. 2014
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