Center for Biophysics and Computational Biology , Department of Chemistry , and Institute for Computational Molecular Science , Temple University , Philadelphia , Pennsylvania 19122 , United States.
Division of Chemical Engineering, Graduate School of Engineering Science , Osaka University , Toyonaka , Osaka 560-8531 , Japan.
J Phys Chem B. 2018 May 3;122(17):4700-4707. doi: 10.1021/acs.jpcb.8b02666. Epub 2018 Apr 23.
We use end point simulations to estimate the excess chemical potential of water in the homogeneous liquid and at the interface with a protein in solution. When the pure liquid is taken as the reference, the excess chemical potential of interfacial water is the difference between the solvation free energy of a water molecule at the interface and in the bulk. Using the homogeneous liquid as an example, we show that the solvation free energy for growing a water molecule can be estimated by applying UWHAM to the simulation data generated from the initial and final states (i.e., "the end points") instead of multistate free energy perturbation simulations because of the possible overlaps of the configurations sampled at the end points. Then end point simulations are used to estimate the solvation free energy of water at the interface with a protein in solution. The estimate of the solvation free energy at the interface from two simulations at the end points agrees with the benchmark using 32 states within a 95% confidence interval for most interfacial locations. The ability to accurately estimate the excess chemical potential of water from end point simulations facilitates the statistical thermodynamic analysis of diverse interfacial phenomena. Our focus is on analyzing the excess chemical potential of water at protein receptor binding sites with the goal of using this information to assist in the design of tight binding ligands.
我们使用终点模拟来估计均匀液相和与溶液中蛋白质界面处水的过剩化学势。当以纯液相为参比时,界面处水的过剩化学势是界面上水分子的溶剂化自由能与体相中的溶剂化自由能之差。以均匀液相为例,我们表明,通过将 UWHAM 应用于从初始和最终状态(即“终点”)生成的模拟数据,可以估计生长水分子的溶剂化自由能,而无需进行多态自由能微扰模拟,因为在终点处采样的构型可能会重叠。然后,使用终点模拟来估计与溶液中蛋白质界面处水的溶剂化自由能。在大多数界面位置,从两个终点模拟中估算的界面溶剂化自由能与使用 32 个状态的基准值在 95%置信区间内一致。从终点模拟准确估计水的过剩化学势的能力促进了对各种界面现象的统计热力学分析。我们的重点是分析蛋白质受体结合位点上水的过剩化学势,目标是利用这些信息来协助设计紧密结合配体。