期刊
FUTURE MEDICINAL CHEMISTRY
卷 10, 期 4, 页码 461-476出版社
FUTURE SCI LTD
DOI: 10.4155/fmc-2017-0172
关键词
CD14; MD-2; natural compounds; structure-activity relationship; synthetic compounds; TLR4
资金
- [H-MSC-ETN-642157]
Activation or inhibition of TLR4 by small molecules will provide in the next few years a new generation of therapeutics. TLR4 stimulation (agonism) by high-affinity ligands mimicking lipid A gave vaccine adjuvants with improved specificity and efficacy that have been licensed and entered into the market. TLR4 inhibition (antagonism) prevents cytokine production at a very early stage; this is in principle a more efficient method to block inflammatory diseases compared to cytokines neutralization by antibodies. Advances in TLR4 modulation by drug-like small molecules achieved in the last years are reviewed. Recently discovered TLR4 agonists and antagonists of natural and synthetic origin are presented, and their mechanism of action and structure-activity relationship are discussed.
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