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

Zaffaroni, L., & Peri, F. (2018). Recent advances on Toll-like receptor 4 modulation: new therapeutic perspectives. FUTURE MEDICINAL CHEMISTRY, 10(4), 461-476 [10.4155/fmc-2017-0172].

Recent advances on Toll-like receptor 4 modulation: new therapeutic perspectives

Zaffaroni, L;Peri, F
2018

Abstract

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
Articolo in rivista - Review Essay
Scientifica
CD14; MD-2; TLR4; natural compounds; structure–activity relationship; synthetic compounds
English
Zaffaroni, L., & Peri, F. (2018). Recent advances on Toll-like receptor 4 modulation: new therapeutic perspectives. FUTURE MEDICINAL CHEMISTRY, 10(4), 461-476 [10.4155/fmc-2017-0172].
Zaffaroni, L; Peri, F
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/10281/185550
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