Madasu Pavan K, Chandran Thyageshwar
Biomolecular Structure and Dynamics Group, Department of Biotechnology, National Institute of Technology, #408, 4th Floor, Warangal, 506004, India.
Arch Toxicol. 2025 Mar;99(3):1143-1152. doi: 10.1007/s00204-024-03927-8. Epub 2024 Dec 13.
Shiga toxin is the leading cause of food poisoning in the world. It is structurally similar to the plant type II ribosome-inactivating proteins (RIPs) and retains N-glycosidase activity. It acts specifically by depurinating the specific adenine A4605 of human 28S rRNA, ultimately inhibiting translation. Recent outbreaks and increasing demands for lab-scale meat assert the necessity for producing toxoids. In the current study, we have carried out the comparative structural and functional analysis of Shiga with ricin for N-glycosidase activity. Primary structural analysis indicates that Shiga is more flexible than ricin and one active site residue Gly121 (ricin), has been mutated to Ser (Shiga). Tertiary structure analysis confirms the conserved active site residue confirmation. Further, molecular dynamic studies indicate that the mutated Ser residue of Shiga imparts flexibility besides interacting with the conserved GAGA loop of 28s rRNA and contributes free energy of -5.39 kcal/mol. We have observed a decreasing trend line of average free binding energy with an average of -23 kcal/mol. The residue interaction network indicates that Arg is the key residue that protonates and initiates the N-glycosidase activity. Overall, these structural studies provide molecular insights into the N-glycosidase mechanism and serve as a prospect for the development of toxoids.
志贺毒素是全球食物中毒的主要原因。它在结构上与植物II型核糖体失活蛋白(RIPs)相似,并保留N-糖苷酶活性。它通过特异性地使人类28S rRNA的特定腺嘌呤A4605脱嘌呤来发挥作用,最终抑制翻译。近期的疫情爆发以及对实验室规模肉类需求的增加,凸显了生产类毒素的必要性。在本研究中,我们对志贺毒素和蓖麻毒素的N-糖苷酶活性进行了比较结构和功能分析。一级结构分析表明,志贺毒素比蓖麻毒素更具灵活性,并且蓖麻毒素的一个活性位点残基Gly121在志贺毒素中已突变为Ser。三级结构分析证实了活性位点残基的保守性。此外,分子动力学研究表明,志贺毒素中突变的Ser残基除了与28s rRNA的保守GAGA环相互作用外,还赋予了灵活性,并贡献了-5.39千卡/摩尔的自由能。我们观察到平均自由结合能呈下降趋势线,平均为-23千卡/摩尔。残基相互作用网络表明,Arg是使N-糖苷酶活性质子化并启动该活性的关键残基。总体而言,这些结构研究为N-糖苷酶机制提供了分子见解,并为类毒素的开发提供了前景。