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Venom-derived modulators of epilepsy-related ion channels

机译：癫痫相关离子通道的毒液衍生调节剂

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Epilepsy is characterised by spontaneous recurrent seizures that are caused by an imbalance between neuronal excitability and inhibition. Since ion channels play fundamental roles in the generation and propagation of action potentials as well as neurotransmitter release at a subset of excitatory and inhibitory synapses, their dysfunction has been linked to a wide variety of epilepsies. Indeed, these unique proteins are the major biological targets for antiepileptic drugs. Selective targeting of a specific ion channel subtype remains challenging for small molecules, due to the high level of homology among members of the same channel family. As a consequence, there is a growing trend to target ion channels with biologics. Venoms are the best known natural source of ion channel modulators, and venom peptides are increasingly recognised as potential therapeutics due to their high selectivity and potency gained through millions of years of evolutionary selection pressure. Here we describe the major ion channel families involved in the pathogenesis of various types of epilepsy, including voltage-gated Na+, K+, Ca2+ channels, Cys-loop receptors, ionotropic glutamate receptors and P2X receptors, and currently available venom-derived peptides that target these channel proteins. Although only a small number of venom peptides have successfully progressed to the clinic, there is reason to be optimistic about their development as antiepileptic drugs, notwithstanding the challenges associated with development of any class of peptide drug.
机译：癫痫是由自发性复发性癫痫发作的特征在于神经元兴奋性和抑制之间的不平衡引起的。由于离子通道在发生和兴奋性和抑制突触的子集中发挥作用和传播的产生和传播的基本作用，因此它们的功能障碍与各种癫痫有关。实际上，这些独特的蛋白质是抗癫痫药物的主要生物学靶标。由于同一渠道家族成员之间的高水平同源性，特定离子通道亚型的选择性靶向对小分子仍然挑战。因此，瞄准具有生物学的离子渠道的日益增长的趋势。毒液是最着名的离子通道调节器的自然来源，毒液肽越来越被认为是由于它们的高选择性和效力，通过数百万多年的进化选择压力而被认为是潜在的治疗剂。在这里，我们描述了参与各种类型的癫痫发病机制的主要离子通道系列，包括电压门控Na +，K +，Ca2 +通道，综合环受体，离子型谷氨酸受体和P2x受体，以及目前可用的毒液衍生的肽这些通道蛋白质。虽然只有少数毒液肽成功地进入诊所，但是，尽管与任何类别肽药物的发育有关的挑战，但是由于任何类别的肽药物的挑战，有理由持乐观。

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