Universidad Nacional Autónoma de México, Instituto de Química, Ciudad Universitaria, Ciudad de México, Mexico.
Institute of Fundamental Technological Research, Polish Academy of Sciences, Warsaw, Poland.
Protein Sci. 2024 Jun;33(6):e5020. doi: 10.1002/pro.5020.
Wheat germ agglutinin (WGA) demonstrates potential as an oral delivery agent owing to its selective binding to carbohydrates and its capacity to traverse biological membranes. In this study, we employed differential scanning calorimetry and molecular dynamics simulations to comprehensively characterize the thermal unfolding process of both the complete lectin and its four isolated domains. Furthermore, we present the nuclear magnetic resonance structures of three domains that were previously lacking experimental structures in their isolated forms. Our results provide a collective understanding of the energetic and structural factors governing the intricate unfolding mechanism of the complete agglutinin, shedding light on the specific role played by each domain in this process. The analysis revealed negligible interdomain cooperativity, highlighting instead significant coupling between dimer dissociation and the unfolding of the more labile domains. By comparing the dominant interactions, we rationalized the stability differences among the domains. Understanding the structural stability of WGA opens avenues for enhanced drug delivery strategies, underscoring its potential as a promising carrier throughout the gastrointestinal environment.
麦胚凝集素(WGA)因其对碳水化合物的选择性结合以及穿透生物膜的能力,显示出作为口服递送剂的潜力。在这项研究中,我们采用差示扫描量热法和分子动力学模拟,全面表征了完整凝集素及其四个分离结构域的热变性过程。此外,我们还展示了三个先前缺乏其分离形式实验结构的结构域的核磁共振结构。我们的研究结果提供了对控制完整凝集素复杂变性机制的能量和结构因素的综合理解,阐明了每个结构域在该过程中的特定作用。分析表明,结构域间的相互协作作用可以忽略不计,而二聚体解离与更不稳定结构域的变性之间存在显著的耦合作用。通过比较主要相互作用,我们可以合理地解释各结构域之间的稳定性差异。对 WGA 结构稳定性的理解为增强药物递送策略开辟了道路,突出了其作为胃肠道环境中一种有前途的载体的潜力。