Cheng Feng, Shen Jianhua, Luo Xiaomin, Jiang Hualiang, Chen Kaixian
Center for Drug Discovery and Design, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 294 Taiyuan Road, Shanghai 200031, Peoples Republic of China.
Biophys J. 2002 Aug;83(2):753-62. doi: 10.1016/S0006-3495(02)75206-5.
The molecular basis of the "tail helix latch" hypothesis in the gelsolin activation process has been studied by using the steered molecular dynamics simulations. In the present nanosecond scale simulations, the tail helix of gelsolin was pulled away from the S2 binding surface, and the required forces were calculated, from which the properties of binding between the tail helix and S2 domain and their dynamic unbinding processes were obtained. The force profile provides a detailed rupture mechanism that includes six major unbinding steps. In particular, the hydrogen bonds formed between Arg-207 and Asp-744 and between Arg-221 and Leu-753 are of the most important interaction pairs. The two hydrogen bond "clamps" stabilize the complex. The subsequent simulation on Arg-207-Ala (R207A) mutation of gelsolin indicated that this mutation facilitates the unbinding of the tail helix and that the contribution of the hydrogen bond between Arg-207 and Asp-744 to the binding is more than 50%, which offers a new clue for further mutagenesis study on the activation mechanism of gelsolin. Surrounding water molecules enhance the stability of the tail helix and facilitate the rupture process. Additionally, temperature also has a significant effect on the conformation of the arginine and arginine-related interactions, which revealed the molecular basis of the temperature dependence in gelsolin activation.
通过使用定向分子动力学模拟研究了凝溶胶蛋白激活过程中“尾螺旋锁”假说的分子基础。在当前的纳秒级模拟中,将凝溶胶蛋白的尾螺旋从S2结合表面拉开,并计算所需的力,由此获得尾螺旋与S2结构域之间的结合特性及其动态解离过程。力曲线提供了一个详细的断裂机制,包括六个主要的解离步骤。特别地,在精氨酸-207与天冬氨酸-744之间以及精氨酸-221与亮氨酸-753之间形成的氢键是最重要的相互作用对。这两个氢键“夹子”稳定了复合物。随后对凝溶胶蛋白的精氨酸-207-丙氨酸(R207A)突变进行的模拟表明,这种突变促进了尾螺旋的解离,并且精氨酸-207与天冬氨酸-744之间的氢键对结合的贡献超过50%,这为进一步对凝溶胶蛋白激活机制进行诱变研究提供了新线索。周围的水分子增强了尾螺旋的稳定性并促进了解离过程。此外,温度对精氨酸及其相关相互作用的构象也有显著影响,这揭示了凝溶胶蛋白激活中温度依赖性的分子基础。