Selective Voltage-Gated Sodium Channel Peptide Toxins from Animal Venom: Pharmacological Probes and Analgesic Drug Development,ACS Chemical Neuroscience

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Selective Voltage-Gated Sodium Channel Peptide Toxins from Animal Venom: Pharmacological Probes and Analgesic Drug Development
ACS Chemical Neuroscience ( IF 4.1 ) Pub Date : 2017-12-08 00:00:00 , DOI: 10.1021/acschemneuro.7b00406
Ying Wu ₁ , Hui Ma ₁ , Fan Zhang ₁ , Chunlei Zhang ₁ , Xiaohan Zou ₁ , Zhengyu Cao ₁

Affiliation

Voltage-gated sodium channels (Navs) play critical roles in action potential generation and propagation. Nav channelopathy as well as pathological sensitization contribute to allodynia and hyperalgesia. Recent evidence has demonstrated the significant roles of Nav subtypes (Nav1.3, 1.7, 1.8, and 1.9) in nociceptive transduction, and therefore these Navs may represent attractive targets for analgesic drug discovery. Animal toxins are structurally diverse peptides that are highly potent yet selective on ion channel subtypes and therefore represent valuable probes to elucidate the structures, gating properties, and cellular functions of ion channels. In this review, we summarize recent advances on peptide toxins from animal venom that selectively target Nav1.3, 1.7, 1.8, and 1.9, along with their potential in analgesic drug discovery.

中文翻译：

来自动物毒液的选择性电压门控钠通道肽毒素：药理探针和止痛药的开发

电压门控钠通道（Navs）在动作电位的产生和传播中起关键作用。Nav通道病以及病理性致敏作用会导致异常性疼痛和痛觉过敏。最近的证据表明，Nav亚型（Nav1.3、1.7、1.8和1.9）在伤害感受转导中具有重要作用，因此这些Navs可能代表镇痛药发现的诱人靶标。动物毒素是结构多样的肽，在离子通道亚型上具有强大的作用力和选择性，因此代表了阐明离子通道的结构，门控特性和细胞功能的有价值的探针。在这篇综述中，我们总结了来自动物毒液的肽毒素的最新进展，这些毒素选择性靶向Nav1.3、1.7、1.8和1.9，以及它们在止痛药发现中的潜力。

更新日期：2017-12-08

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