The DOI matches its Crossref record; 115 of the 115 references it cites were found in a registry or an index.
Toll-like receptor 4 (TLR4) inhibitors: Current research and prospective
Open accessAbstract
Toll-like receptor 4 (TLR4), a member of the Toll-like receptor (TLR) family, is involved in innate immunity and mediates inflammatory responses by recognizing lipopolysaccharide (LPS) or bacterial endotoxins. Hyperactivation of TLR4 triggers the production of various inflammatory factors, which are associated with the development of a variety of diseases, such as sepsis, endotoxemia, acute lung injury, rheumatoid arthritis, and cardiovascular diseases. And anti-inflammatory potential of TLR4 inhibitors have been validated. In this review, we discuss TLR4 inhibitors that can bind directly to TLR4 or the TLR4/MD2 complex, and provide a brief introduction to compounds that can downregulate the expression of TLR4. We focused on the possible modes by which the TLR4 inhibitors bind to the TLR4 or TLR4/MD2 complex. Three compounds targeting TLR4 have entered clinical trials, but unfortunately, two of them have been discontinued due to poor efficacy. Therefore, the discovery of effective small molecular compounds is the main research focus for TLR4 inhibitor design. In this review, by summarizing results from molecular dynamics simulation and molecular docking, we found that the Arg241 residue of TLR4 and the Tyr102, Ser120, and Lys122 residues of MD2 are involved in the binding of antagonistic ligands to the TLR4/MD2 complex; this is useful information for structure-based TLR4 inhibitor design.
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Cites
The role of pattern-recognition receptors in innate immunity: update on Toll-like receptors
Kawai, T., & Akira, S. (2010) · Nature Immunology · doi:10.1038/ni.1863 · Cited by 9,304
Phosphorylation meets ubiquitination: the control of NF-κB activity
Karin, M., & Ben-Neriah, Y. (2000) · Annual Review of Immunology · doi:10.1146/annurev.immunol.18.1.621 · Cited by 4,766
The structural basis of lipopolysaccharide recognition by the TLR4–MD-2 complex
Park, B. S., Song, D. H., Kim, H. M., Choi, B.-S., Lee, H., & Lee, J.-O. (2009) · Nature · doi:10.1038/nature07830 · Cited by 2,428
Phosphorylation of innate immune adaptor proteins MAVS, STING, and TRIF induces IRF3 activation
Liu, S., Cai, X., Wu, J., Cong, Q., Chen, X., Li, T., Du, F., Ren, J., Wu, Y.-T., Grishin, N. V., et al. (2015) · Science · doi:10.1126/science.aaa2630 · Cited by 1,927
The history of toll-like receptors - redefining innate immunity
O'Neill, L. A. J., Golenbock, D., & Bowie, A. G. (2013) · Nature reviews. Immunology · doi:10.1038/nri3446 · Cited by 1,765
Collins, T., Read, M. A., Neish, A. S., Whitley, M. Z., Thanos, D., & Maniatis, T. (1995) · The FASEB Journal · doi:10.1096/fasebj.9.10.7542214 · Cited by 1,718
TLR4 and CD14 trafficking and its influence on LPS-induced pro-inflammatory signaling
Ciesielska, A., Matyjek, M., & Kwiatkowska, K. (2021) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-020-03656-y · Cited by 1,420
Regulation of lung injury and repair by Toll-like receptors and hyaluronan
Jiang, D., Liang, J., Fan, J., Yu, S., Chen, S., Luo, Y., Prestwich, G. D., Mascarenhas, M. M., Garg, H. G., Quinn, D. A., et al. (2005) · Nature Medicine · doi:10.1038/nm1315 · Cited by 1,401
Mal (MyD88-adapter-like) is required for Toll-like receptor-4 signal transduction
Fitzgerald, K. A., Palsson-McDermott, E. M., Bowie, A. G., Jefferies, C. A., Mansell, A. S., Brady, G., Brint, E., Dunne, A., Gray, P., Harte, M. T., et al. (2001) · Nature · doi:10.1038/35092578 · Cited by 1,256
Crystal Structure of the TLR4-MD-2 Complex with Bound Endotoxin Antagonist Eritoran
Kim, H. M., Park, B. S., Kim, J.-I., Kim, S. E., Lee, J., Oh, S. C., Enkhbayar, P., Matsushima, N., Lee, H., Yoo, O. J., et al. (2007) · Cell · doi:10.1016/j.cell.2007.08.002 · Cited by 1,177
Cited by
Toll-like receptor 4: A potential therapeutic target for multiple human diseases
Wei, J., Zhang, Y., Li, H., Wang, F., & Yao, S. (2023) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2023.115338 · Cited by 121
Self-citationTu, Y., Liu, J., Kong, D., Guo, X., Li, J., Long, Z., Peng, J., Wang, Z., Wu, H., Liu, P., et al. (2023) · Free Radical Biology and Medicine · doi:10.1016/j.freeradbiomed.2023.03.014 · Cited by 89
Jin, L., Cui, Y., Zhang, Q., Xiong, Y., Zheng, X., Ye, J., Zhang, A., Xiao, Z., Zhuang, Z., Liang, G., et al. (2025) · International Immunopharmacology · doi:10.1016/j.intimp.2025.114053 · Cited by 1
Metadata
- Authors
- Zhang, Y., Liang, X., Bao, X., Xiao, W., & Chen, G.
- Venue
- European Journal of Medicinal Chemistry
- Publisher
- Elsevier BV
- Published
- 2022-05
- Volume
- 235
- Pages
- 114291
- ISSN
- 0223-5234 (ISSN-L)
- OpenAlex
- W4220961657
- Cited by
- 299
- References
- 115
- FWCI
- 19.04
- Type
- journal article
- Language
- en
- Open access
- green
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- Zhang, Y., Liang, X., Bao, X., Xiao, W., & Chen, G. (2022). Toll-like receptor 4 (TLR4) inhibitors: Current research and prospective. European Journal of Medicinal Chemistry. https://doi.org/10.1016/j.ejmech.2022.114291
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