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Cnidarian peptide neurotoxins: a new source of various ion channel modulators or blockers against central nervous systems disease
Drug Discovery Today ( IF 6.5 ) Pub Date : 2018-08-27 , DOI: 10.1016/j.drudis.2018.08.011
Qiwen Liao , Yu Feng , Binrui Yang , Simon Ming-Yuen Lee

Cnidaria provide the largest source of bioactive peptides for new drug development. The venoms contain enzymes, potent pore-forming toxins and neurotoxins. The neurotoxins can immobilize predators rapidly when discharged via modifying sodium-channel-gating or blocking the potassium channel during the repolarization stage. Most cnidarian neurotoxins remain conserved under the strong influence of negative selection. Neuroactive peptides targeting the central nervous system through affinity with ion channels could provide insight leading to drug treatment of neurological diseases, which arise from ion channel dysfunctions. Although marine resources offer thousands of possible peptides, only one peptide derived from Cnidaria: ShK-186, also named dalazatide, has reached the pharmaceutical market. This review focuses on neuroprotective agents derived from cnidarian neurotoxic peptides.



中文翻译:

念头肽神经毒素:抗中枢神经系统疾病的各种离子通道调节剂或阻断剂的新来源

刺鼻为新药开发提供了最大的生物活性肽来源。毒液包含酶,有效的造孔毒素和神经毒素。当在复极化阶段通过修饰钠通道门控或阻断钾通道排出时,神经毒素可以快速固定捕食者。在负选择的强烈影响下,大多数cnidarian神经毒素仍保持保守。通过与离子通道的亲和力靶向中枢神经系统的神经活性肽可以提供见识,从而导致对由离子通道功能障碍引起的神经系统疾病进行药物治疗。尽管海洋资源提供了成千上万种可能的肽,但只有一种源自猪唇草的肽:ShK-186,也称为达拉沙肽,已进入制药市场。

更新日期:2018-08-27
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