REV-ERB activation as a novel pharmacological approach for treating inflammatory pain.
REV-ERB activation as a novel pharmacological approach for treating inflammatory pain.
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DOI：
10.3389/fphar.2023.1171931
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发表时间：
2023
影响因子：
5.6
通讯作者：
中科院分区：
文献类型：
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作者：
疼痛是一个复杂的问题，影响着全世界数百万人。目前用于减轻疼痛的疗法是有限的，因为许多治疗选择不足以解决疼痛的原因，导致药物耐受性，或具有包括滥用可能性的不良反应。虽然疼痛的原因有很多，但疼痛病症的发病机制和维持的一个潜在机制是由NLRP 3炎性体驱动的慢性炎症。目前正在研究几种炎性体抑制剂，但它们有可能抑制先天免疫系统的功能，这可能会对患者造成不必要的影响。在这里，我们表明，核受体REV-ERB可以抑制激活的炎性小体时，小分子激动剂激活。此外，REV-ERB激活似乎在急性炎性疼痛模型中具有镇痛潜力，这可能是炎性小体抑制的结果。
Pain is a complex problem affecting millions of people worldwide. The current therapies to reduce pain are limited as many treatment options inadequately address the causes of pain, lead to tolerance of the drug, or have adverse effects including abuse potential. While there are many causes of pain, one underlying mechanism to the pathogenesis and maintenance of pain conditions is chronic inflammation driven by the NLRP3 inflammasome. Several inflammasome inhibitors are currently under investigation however have the potential to suppress the functioning of the innate immune system, which may cause unwanted affects in patients. Here, we show that the nuclear receptor REV-ERB can suppress the activation of the inflammasome when pharmacologically activated with small molecule agonists. Additionally, REV-ERB activation appears to have analgesic potential in a model of acute inflammatory pain, likely as a result of inflammasome suppression.
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DOI：
10.1523/jneurosci.3295-09.2010
发表时间：
2010-01-13
期刊：
The Journal of neuroscience : the official journal of the Society for Neuroscience
影响因子：
--
作者：
Clark AK;Staniland AA;Marchand F;Kaan TK;McMahon SB;Malcangio M
通讯作者：
Malcangio M
影响因子：
5.8
作者：
Hong, Huiling;Cheung, Yiu Ming;Tian, Xiao Yu
通讯作者：
Tian, Xiao Yu
影响因子：
29.4
作者：
Pourcet B;Zecchin M;Ferri L;Beauchamp J;Sitaula S;Billon C;Delhaye S;Vanhoutte J;Mayeuf-Louchart A;Thorel Q;Haas JT;Eeckhoute J;Dombrowicz D;Duhem C;Boulinguiez A;Lancel S;Sebti Y;Burris TP;Staels B;Duez HM
通讯作者：
Duez HM
影响因子：
16.6
作者：
Murray, Meghan H.;Valfort, Aurore Cecile;Koelblen, Thomas;Ronin, Celine;Ciesielski, Fabrice;Chatterjee, Arindam;Veerakanellore, Giri Babu;Elgendy, Bahaa;Walker, John K.;Hegazy, Lamees;Burris, Thomas P.
通讯作者：
Burris, Thomas P.
影响因子：
16.6
作者：
Banerjee, Subhashis;Wang, Yongjun;Burris, Thomas P.
通讯作者：
Burris, Thomas P.