• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

来自罗氏芋螺的N端延长肽定义了一类靶向肌肉型烟碱乙酰胆碱受体的新型带状α-芋螺毒素。

An N-Terminally Elongated Peptide From Conus rolani Defines a New Class of Ribbon α-Conotoxins Targeting Muscle nAChRs.

作者信息

Giglio Matías L, Flórez-Salcedo Paula, Azam Layla, Watkins Maren, Koch Thomas Lund, Basgall-De la Rosa Erianna, Douglass Adam D, McIntosh J Michael, Olivera Baldomero M, Gajewiak Joanna

机构信息

School of Biological Sciences, University of Utah, Salt Lake City, Utah, USA.

Department of Biochemistry, University of Utah, Salt Lake City, Utah, USA.

出版信息

FASEB J. 2025 Jun 30;39(12):e70698. doi: 10.1096/fj.202500721RR.

DOI:10.1096/fj.202500721RR
PMID:40536237
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12178101/
Abstract

Conotoxins, peptides found in cone snail venoms, selectively target ion channels and receptors to incapacitate prey. α-Conotoxins are extensively investigated for their potent modulation of nicotinic acetylcholine receptors (nAChRs). This study describes the discovery and characterization of RoIA, a novel α-conotoxin from Conus rolani. RoIA belongs to the α4/4 conotoxin class and features an atypical N-terminal elongation of 18 amino acids. The biological activity of RoIA is assessed through both in vivo and in vitro assays using the three potential folding isoforms (globular, ribbon, and bead) of the full-length and truncated (lacking the N-terminal elongation) analogs. The full-length RoIA analog exhibits delayed but potent paralytic activity when administered to mice and fish; the ribbon isoform shows the highest potency. Notably, only the ribbon isoform of the truncated peptide is active on heterologously expressed muscle nAChRs, suggesting that the N-terminal elongation may be released in vivo or form interactions that are not recapitulated in vitro. This discovery challenges the prevailing understanding that native α-conotoxins adopt a globular conformation and illustrates that Conus can explore novel chemical spaces using an alternative disulfide bond connectivity. This research enhances our knowledge of the complex mechanisms by which toxins manifest their physiological effects.

摘要

芋螺毒素是在芋螺毒液中发现的肽类物质,它们能选择性地作用于离子通道和受体,使猎物丧失活动能力。α-芋螺毒素因其对烟碱型乙酰胆碱受体(nAChRs)的强效调节作用而受到广泛研究。本研究描述了一种来自罗氏芋螺的新型α-芋螺毒素RoIA的发现与特性。RoIA属于α4/4芋螺毒素类别,其特点是N端有18个氨基酸的非典型延长。通过体内和体外实验,利用全长及截短(缺少N端延长部分)类似物的三种潜在折叠异构体(球状、带状和珠状)评估了RoIA的生物活性。将全长RoIA类似物注射到小鼠和鱼类体内时,会表现出延迟但强效的麻痹活性;带状异构体的效力最高。值得注意的是,截短肽只有带状异构体对异源表达的肌肉nAChRs有活性,这表明N端延长部分可能在体内被释放,或者形成了体外无法重现的相互作用。这一发现挑战了天然α-芋螺毒素采用球状构象的主流认知,并表明芋螺可以利用另一种二硫键连接方式探索新的化学空间。这项研究增进了我们对毒素发挥生理效应的复杂机制的了解。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/d20d88fdd974/FSB2-39-e70698-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/6089abb3cbbf/FSB2-39-e70698-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/fbe448404f2f/FSB2-39-e70698-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/f26209bbecb8/FSB2-39-e70698-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/ce1280651782/FSB2-39-e70698-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/cbd17106c05a/FSB2-39-e70698-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/ed8ee71300a1/FSB2-39-e70698-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/6192e76c42a3/FSB2-39-e70698-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/d20d88fdd974/FSB2-39-e70698-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/6089abb3cbbf/FSB2-39-e70698-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/fbe448404f2f/FSB2-39-e70698-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/f26209bbecb8/FSB2-39-e70698-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/ce1280651782/FSB2-39-e70698-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/cbd17106c05a/FSB2-39-e70698-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/ed8ee71300a1/FSB2-39-e70698-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/6192e76c42a3/FSB2-39-e70698-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8d7/12178101/d20d88fdd974/FSB2-39-e70698-g001.jpg

相似文献

1
An N-Terminally Elongated Peptide From Conus rolani Defines a New Class of Ribbon α-Conotoxins Targeting Muscle nAChRs.来自罗氏芋螺的N端延长肽定义了一类靶向肌肉型烟碱乙酰胆碱受体的新型带状α-芋螺毒素。
FASEB J. 2025 Jun 30;39(12):e70698. doi: 10.1096/fj.202500721RR.
2
Globular and ribbon isomers of Conus geographus α-conotoxins antagonize human nicotinic acetylcholine receptors.芋螺 α-芋螺毒素的球形和带状异构体拮抗人烟碱型乙酰胆碱受体。
Biochem Pharmacol. 2021 Aug;190:114638. doi: 10.1016/j.bcp.2021.114638. Epub 2021 May 29.
3
Discovery of a new subclass of α-conotoxins in the venom of Conus australis.在澳大利亚芋螺毒液中发现α-芋螺毒素的一个新亚类。
Toxicon. 2014 Dec;91:145-54. doi: 10.1016/j.toxicon.2014.08.074. Epub 2014 Sep 4.
4
Rigidity of loop 1 contributes to equipotency of globular and ribbon isomers of α-conotoxin AusIA.环 1 的刚性有助于 α-芋螺毒素 AusIA 的球形和带状异构体的等势能。
Sci Rep. 2021 Nov 9;11(1):21928. doi: 10.1038/s41598-021-01277-4.
5
A short framework-III (mini-M-2) conotoxin from the venom of a vermivorous species, Conus archon, inhibits human neuronal nicotinic acetylcholine receptors.一种来自食虫种 Conus archon 毒液的短框架-III(迷你-M-2)芋螺毒素,抑制人类神经元烟碱型乙酰胆碱受体。
Peptides. 2022 Jul;153:170785. doi: 10.1016/j.peptides.2022.170785. Epub 2022 Mar 17.
6
Novel alpha-conotoxins from Conus spurius and the alpha-conotoxin EI share high-affinity potentiation and low-affinity inhibition of nicotinic acetylcholine receptors.来自螺旋锥螺的新型α-芋螺毒素与α-芋螺毒素EI对烟碱型乙酰胆碱受体具有高亲和力增强作用和低亲和力抑制作用。
FEBS J. 2007 Aug;274(15):3972-85. doi: 10.1111/j.1742-4658.2007.05931.x. Epub 2007 Jul 16.
7
Structure-Function Elucidation of a New α-Conotoxin, MilIA, from .阐明一种新型α-芋螺毒素 MilIA 的结构与功能
Mar Drugs. 2019 Sep 16;17(9):535. doi: 10.3390/md17090535.
8
A novel conotoxin inhibitor of Kv1.6 channel and nAChR subtypes defines a new superfamily of conotoxins.一种新型的Kv1.6通道和烟碱型乙酰胆碱受体亚型的芋螺毒素抑制剂定义了一个新的芋螺毒素超家族。
Biochemistry. 2006 Jul 11;45(27):8331-40. doi: 10.1021/bi060263r.
9
Research into the Bioengineering of a Novel α-Conotoxin from the Milked Venom of .研究从. 的毒液中提取新型 α-芋螺毒素的生物工程学。
Int J Mol Sci. 2022 Oct 11;23(20):12096. doi: 10.3390/ijms232012096.
10
Isolation and characterization of α-conotoxin LsIA with potent activity at nicotinic acetylcholine receptors.分离和鉴定具有烟碱型乙酰胆碱受体活性的α-芋螺毒素 LsIA。
Biochem Pharmacol. 2013 Sep 15;86(6):791-9. doi: 10.1016/j.bcp.2013.07.016. Epub 2013 Aug 4.

本文引用的文献

1
χ-Conotoxins are an Evolutionary Innovation of Mollusk-Hunting Cone Snails as a Counter-Adaptation to Prey Defense.χ-芋螺毒素是捕食软体动物的芋螺在进化过程中的创新,作为对猎物防御的一种反适应。
Mol Biol Evol. 2024 Nov 1;41(11). doi: 10.1093/molbev/msae226.
2
Elucidation of Medusozoan (Jellyfish) Venom Constituent Activities Using Constellation Pharmacology.利用星座药理学阐明水螅虫类(水母)毒液成分的活性。
Toxins (Basel). 2024 Oct 17;16(10):447. doi: 10.3390/toxins16100447.
3
Prey Shifts Drive Venom Evolution in Cone Snails.猎物转移驱动圆锥蜗牛毒液进化。
Mol Biol Evol. 2024 Aug 2;41(8). doi: 10.1093/molbev/msae120.
4
Using Constellation Pharmacology to Characterize a Novel α-Conotoxin from .利用星座药理学研究一种新型α-芋螺毒素。
Mar Drugs. 2024 Feb 29;22(3):118. doi: 10.3390/md22030118.
5
Synthesis and Biological Activity of Novel α-Conotoxins Derived from Endemic Polynesian Cone Snails.新型来源于特有波利尼西亚芋螺的α-Conotoxin 的合成与生物活性。
Mar Drugs. 2023 Jun 9;21(6):356. doi: 10.3390/md21060356.
6
Discovery, Characterization, and Engineering of LvIC, an α4/4-Conotoxin That Selectively Blocks Rat α6/α3β4 Nicotinic Acetylcholine Receptors.LvIC 的发现、鉴定与工程改造:一种选择性阻断大鼠 α6/α3β4 烟碱型乙酰胆碱受体的 α4/4-芋螺毒素。
J Med Chem. 2023 Feb 9;66(3):2020-2031. doi: 10.1021/acs.jmedchem.2c01786. Epub 2023 Jan 22.
7
Modern venomics-Current insights, novel methods, and future perspectives in biological and applied animal venom research.现代毒液学——生物和应用动物毒液研究的当前见解、新方法和未来展望。
Gigascience. 2022 May 18;11. doi: 10.1093/gigascience/giac048.
8
Cysteine-Rich α-Conotoxin SII Displays Novel Interactions at the Muscle Nicotinic Acetylcholine Receptor.富含半胱氨酸的α-芋螺毒素SII在肌肉烟碱型乙酰胆碱受体上表现出新型相互作用。
ACS Chem Neurosci. 2022 Apr 20;13(8):1245-1250. doi: 10.1021/acschemneuro.1c00857. Epub 2022 Mar 31.
9
Somatostatin venom analogs evolved by fish-hunting cone snails: From prey capture behavior to identifying drug leads.鱼猎芋螺衍生的生长抑素类似物:从猎物捕获行为到药物先导物的鉴定。
Sci Adv. 2022 Mar 25;8(12):eabk1410. doi: 10.1126/sciadv.abk1410. Epub 2022 Mar 23.
10
Rigidity of loop 1 contributes to equipotency of globular and ribbon isomers of α-conotoxin AusIA.环 1 的刚性有助于 α-芋螺毒素 AusIA 的球形和带状异构体的等势能。
Sci Rep. 2021 Nov 9;11(1):21928. doi: 10.1038/s41598-021-01277-4.