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海葵:在肽毒素领域的无声成就者。

Sea Anemones: Quiet Achievers in the Field of Peptide Toxins.

机构信息

School of Earth, Environmental and Biological Sciences, Queensland University of Technology (QUT), Brisbane, QLD 4001, Australia.

Institute of Future Environments, Queensland University of Technology (QUT), Brisbane, QLD 4001, Australia.

出版信息

Toxins (Basel). 2018 Jan 8;10(1):36. doi: 10.3390/toxins10010036.

Abstract

Sea anemones have been understudied as a source of peptide and protein toxins, with relatively few examined as a source of new pharmacological tools or therapeutic leads. This is surprising given the success of some anemone peptides that have been tested, such as the potassium channel blocker from known as ShK. An analogue of this peptide, ShK-186, which is now known as dalazatide, has successfully completed Phase 1 clinical trials and is about to enter Phase 2 trials for the treatment of autoimmune diseases. One of the impediments to the exploitation of sea anemone toxins in the pharmaceutical industry has been the difficulty associated with their high-throughput discovery and isolation. Recent developments in multiple 'omic' technologies, including genomics, transcriptomics and proteomics, coupled with advanced bioinformatics, have opened the way for large-scale discovery of novel sea anemone toxins from a range of species. Many of these toxins will be useful pharmacological tools and some will hopefully prove to be valuable therapeutic leads.

摘要

海葵作为肽和蛋白质毒素的来源一直研究不足,作为新药理学工具或治疗靶点的来源的研究相对较少。考虑到一些已测试的海葵肽取得了成功,这令人感到惊讶,例如已知的钾通道阻滞剂 ShK。这种肽的类似物 ShK-186,现在称为 dalazatide,已成功完成了 1 期临床试验,即将进入 2 期临床试验,用于治疗自身免疫性疾病。海葵毒素在制药行业中难以得到充分利用的一个障碍是与它们的高通量发现和分离相关的困难。多种“组学”技术(包括基因组学、转录组学和蛋白质组学)的最新发展,加上先进的生物信息学,为从多种物种中大规模发现新型海葵毒素开辟了道路。其中许多毒素将是有用的药理学工具,有些则有望成为有价值的治疗靶点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b872/5793123/3d038edb3bf1/toxins-10-00036-g001.jpg

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