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神经毒素毒液肽治疗学。

Conotoxin venom peptide therapeutics.

机构信息

Xenome Ltd, Indooroopilly 4068 and Institute for Molecular Biosciences, The University of Queensland, 4072, Brisbane, Australia.

出版信息

Adv Exp Med Biol. 2009;655:44-8. doi: 10.1007/978-1-4419-1132-2_5.

Abstract

Venom peptides offer enormous opportunity for the discovery of peptide drug leads. This review focusses on the potential of cone snails that have developed arrays of small peptides as part of highly evolved venoms used for prey capture and defence. Many of these peptides selectively modulate ion channels and transporters, making them a valuable source of new ligands for studying the role these targets play in normal and disease physiology. A number of these conopeptides reduce pain in animals models and several are now in preclinical and clinical development for the treatment of severe pain often associated with diseases such as cancer.

摘要

毒液肽为发现肽类药物先导物提供了巨大的机会。本综述重点介绍了作为高度进化毒液的一部分而开发出的一系列小肽的圆锥蜗牛的潜力,这些毒液用于猎物捕获和防御。这些肽中的许多都选择性地调节离子通道和转运蛋白,使它们成为研究这些靶标在正常和疾病生理中作用的新配体的宝贵来源。其中一些芋螺毒素在动物模型中能减轻疼痛,并且有几种目前正在进行临床前和临床开发,用于治疗与癌症等疾病相关的严重疼痛。

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