Discovery and development of voltage-gated sodium channel inhibitors

电压门控钠通道抑制剂的发现和开发

• 批准号: 10487119
• 负责人: Ingrid Schroeder
• 金额: $ 10.66万
• 依托单位: DIVISION OF BASIC SCIENCES - NCI
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/10487119
• 关键词: Animals; Cone; Development; Genetic; Ion Channel Gating; Pain; Peptides; Research; Role; Snails; Sodium Channel; Spider Venoms; Toxin; Treatment-Related Cancer; chronic neuropathic pain; in vivo; inhibitor/antagonist; novel; painful neuropathy; voltage

The role of voltage-gated sodium channels in pain propagation is indisputable with mounting genetic evidence of sodium channel subtypes NaV1.7-NaV1.9 specifically being involved. Animal toxins are known to target voltage-gated ion channels at high potency and often with exquisite subtype selectivity. Our research focuses on identifying and developing novel sodium channel NaV1.7 selective peptides from the venom of spiders and cone snails to develop novel NaV1.7 inhibitors for the treatment of cancer-associated neuropathic pain.

电压门控钠通道在疼痛传播中的作用是毋庸置疑的，越来越多的遗传证据表明钠通道亚型Nav1.7-NaV1.9具体参与其中。众所周知，动物毒素以高效的电压门控离子通道为靶标，并且往往具有精致的亚型选择性。我们的研究集中在从蜘蛛和锥形蜗牛的毒液中寻找和开发新的钠通道Nav1.7选择性多肽，以开发用于治疗癌症相关神经病理性疼痛的新型Nav1.7抑制剂。