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
School of Biological Sciences, University of Utah, Salt Lake City, Utah, USA.
Department of Biochemistry, University of Utah, Salt Lake City, Utah, USA.
FASEB J. 2025 Jun 30;39(12):e70698. doi: 10.1096/fj.202500721RR.
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.
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。