Pineda Sandy S, Undheim Eivind A B, Rupasinghe Darshani B, Ikonomopoulou Maria P, King Glenn F
Institute for Molecular Bioscience, University of Queensland, Queensland, Australia.
Future Med Chem. 2014 Oct;6(15):1699-714. doi: 10.4155/fmc.14.103.
Over a period of more than 300 million years, spiders have evolved complex venoms containing an extraordinary array of toxins for prey capture and defense against predators. The major components of most spider venoms are small disulfide-bridged peptides that are highly stable and resistant to proteolytic degradation. Moreover, many of these peptides have high specificity and potency toward molecular targets of therapeutic importance. This unique combination of bioactivity and stability has made spider-venom peptides valuable both as pharmacological tools and as leads for drug development. This review describes recent advances in spider-venom-based drug discovery pipelines. We discuss spider-venom-derived peptides that are currently under investigation for treatment of a diverse range of pathologies including pain, stroke and cancer.
在超过3亿年的时间里，蜘蛛进化出了复杂的毒液，其中含有一系列用于捕食猎物和抵御捕食者的特殊毒素。大多数蜘蛛毒液的主要成分是小的二硫键连接的肽，这些肽高度稳定，对蛋白水解降解具有抗性。此外，这些肽中的许多对具有治疗重要性的分子靶点具有高特异性和效力。这种生物活性和稳定性的独特组合使蜘蛛毒液肽作为药理学工具和药物开发的先导都具有价值。本综述描述了基于蜘蛛毒液的药物发现流程的最新进展。我们讨论了目前正在研究用于治疗包括疼痛、中风和癌症在内的多种病症的蜘蛛毒液衍生肽。
