Receptor and channel heteromers as pain targets.
Receptor and channel heteromers as pain targets.
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DOI：
10.3390/ph5030249
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发表时间：
2012-02-23
期刊：
影响因子：
--
通讯作者：
Akopian AN
中科院分区：
文献类型：
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作者：
Berg KA;Patwardhan AM;Akopian AN
最近的发现表明，许多参与疼痛调节的 G 蛋白偶联受体 (GPCR) 和通道能够形成受体异聚体。与单体/同聚体受体或离子通道对应物相比，受体和通道异聚体通常表现出不同的信号传导特征、药理学特性和生理功能。或许可以利用这种独特的特性来增强治疗效果，同时最大限度地减少副作用。例如，专门针对异聚体的药物可能具有更大的组织特异性和镇痛功效。本综述将重点关注目前我们对异聚 GPCR 和通道在疼痛通路中的作用的理解进展，以及通过靶向异聚受体和通道来控制疼痛通路的策略。这种方法可能有助于发现新型药物并扩大我们的疼痛药物治疗靶点。
Recent discoveries indicate that many G-protein coupled receptors (GPCRs) and channels involved in pain modulation are able to form receptor heteromers. Receptor and channel heteromers often display distinct signaling characteristics, pharmacological properties and physiological function in comparison to monomer/homomer receptor or ion channel counterparts. It may be possible to capitalize on such unique properties to augment therapeutic efficacy while minimizing side effects. For example, drugs specifically targeting heteromers may have greater tissue specificity and analgesic efficacy. This review will focus on current progress in our understanding of roles of heteromeric GPCRs and channels in pain pathways as well as strategies for controlling pain pathways via targeting heteromeric receptors and channels. This approach may be instrumental in the discovery of novel classes of drugs and expand our repertoire of targets for pain pharmacotherapy.