International Research Centre for Nano Handling and Manufacturing of China, Changchun University of Science and Technology, Changchun, 130022, China.
Ministry of Education Key Laboratory for Cross-Scale Micro and Nano Manufacturing, Changchun University of Science and Technology, Changchun, 130022, China.
Sci Rep. 2024 Apr 4;14(1):7975. doi: 10.1038/s41598-024-58584-9.
Alzheimer's disease (AD) presents a significant challenge in neurodegenerative disease management, with limited therapeutic options available for its prevention and treatment. At the heart of AD pathogenesis is the amyloid-β (Aβ) protein precursor (APP), with the interaction between APP and the adaptor protein Mint2 being crucial. Despite previous explorations into the APP-Mint2 interaction, the dynamic regulatory mechanisms by which Mint2 modulates APP binding remain poorly understood. This study undertakes molecular dynamics simulations across four distinct systems-free Mint2, Mint2 bound to APP, a mutant form of Mint2, and the mutant form bound to APP-over an extensive 400 ns timeframe. Our findings reveal that the mutant Mint2 experiences significant secondary structural transformations, notably the formation of an α-helix in residues S55-K65 upon APP binding, within the 400 ns simulation period. Additionally, we observed a reduction in the active pocket size of the mutant Mint2 compared to its wild-type counterpart, enhancing its APP binding affinity. These insights hold promise for guiding the development of novel inhibitors targeting the Mints family, potentially paving the way for new therapeutic strategies in AD prevention and treatment.
阿尔茨海默病(AD)是神经退行性疾病管理中的一个重大挑战,目前可用于预防和治疗 AD 的治疗方法有限。AD 发病机制的核心是淀粉样蛋白-β(Aβ)蛋白前体(APP),APP 与衔接蛋白 Mint2 之间的相互作用至关重要。尽管之前已经探索了 APP-Mint2 相互作用,但 Mint2 调节 APP 结合的动态调节机制仍知之甚少。本研究通过四个不同系统(无 Mint2、与 APP 结合的 Mint2、突变型 Mint2 和与 APP 结合的突变型 Mint2)进行了长达 400ns 的分子动力学模拟。我们的研究结果表明,在 400ns 的模拟过程中,突变型 Mint2 经历了显著的二级结构转变,特别是在与 APP 结合后,残基 S55-K65 形成了一个α-螺旋。此外,与野生型相比,突变型 Mint2 的活性口袋尺寸减小,从而增强了其与 APP 的结合亲和力。这些发现为开发针对 Mints 家族的新型抑制剂提供了指导,可能为 AD 的预防和治疗开辟新的治疗策略。