Laboratory for Biomolecular Simulation Research, Institute for Quantitative Biomedicine, and Department of Chemistry and Chemical Biology, Rutgers the State University of New Jersey, New Brunswick, New Jersey 08901-8554, United States.
J Chem Theory Comput. 2021 Nov 9;17(11):6993-7009. doi: 10.1021/acs.jctc.1c00201. Epub 2021 Oct 13.
We develop a new deep potential─range correction (DPRc) machine learning potential for combined quantum mechanical/molecular mechanical (QM/MM) simulations of chemical reactions in the condensed phase. The new range correction enables short-ranged QM/MM interactions to be tuned for higher accuracy, and the correction smoothly vanishes within a specified cutoff. We further develop an active learning procedure for robust neural network training. We test the DPRc model and training procedure against a series of six nonenzymatic phosphoryl transfer reactions in solution that are important in mechanistic studies of RNA-cleaving enzymes. Specifically, we apply DPRc corrections to a base QM model and test its ability to reproduce free-energy profiles generated from a target QM model. We perform these comparisons using the MNDO/d and DFTB2 semiempirical models because they differ in the way they treat orbital orthogonalization and electrostatics and produce free-energy profiles which differ significantly from each other, thereby providing us a rigorous stress test for the DPRc model and training procedure. The comparisons show that accurate reproduction of the free-energy profiles requires correction of the QM/MM interactions out to 6 Å. We further find that the model's initial training benefits from generating data from temperature replica exchange simulations and including high-temperature configurations into the fitting procedure, so the resulting models are trained to properly avoid high-energy regions. A single DPRc model was trained to reproduce four different reactions and yielded good agreement with the free-energy profiles made from the target QM/MM simulations. The DPRc model was further demonstrated to be transferable to 2D free-energy surfaces and 1D free-energy profiles that were not explicitly considered in the training. Examination of the computational performance of the DPRc model showed that it was fairly slow when run on CPUs but was sped up almost 100-fold when using NVIDIA V100 GPUs, resulting in almost negligible overhead. The new DPRc model and training procedure provide a potentially powerful new tool for the creation of next-generation QM/MM potentials for a wide spectrum of free-energy applications ranging from drug discovery to enzyme design.
我们开发了一种新的深度势能-范围修正(DPRc)机器学习势能,用于在凝聚相中进行化学反应的量子力学/分子力学(QM/MM)模拟。新的范围修正能够调整短程 QM/MM 相互作用以获得更高的准确性,并且修正在指定的截止值内平滑地消失。我们进一步开发了一种用于稳健神经网络训练的主动学习程序。我们通过一系列在溶液中非酶促磷酸转移反应来测试 DPRc 模型和训练程序,这些反应对于 RNA 切割酶的机制研究很重要。具体来说,我们将 DPRc 修正应用于基本 QM 模型,并测试其从目标 QM 模型生成的自由能曲线的能力。我们使用 MNDO/d 和 DFTB2 半经验模型进行这些比较,因为它们在处理轨道正交化和静电的方式上有所不同,并且产生的自由能曲线彼此之间存在显著差异,从而为 DPRc 模型和训练程序提供了严格的压力测试。比较表明,准确再现自由能曲线需要修正 QM/MM 相互作用至 6 Å。我们还发现,模型的初始训练受益于从温度交换模拟中生成数据并将高温构象纳入拟合过程,因此所得到的模型经过训练可以正确避免高能区域。一个单一的 DPRc 模型被训练来再现四个不同的反应,并与从目标 QM/MM 模拟生成的自由能曲线很好地吻合。进一步证明 DPRc 模型可转移到未在训练中明确考虑的 2D 自由能表面和 1D 自由能曲线。对 DPRc 模型的计算性能进行检查表明,它在 CPU 上运行时相当缓慢,但在使用 NVIDIA V100 GPU 时速度提高了近 100 倍,几乎没有开销。新的 DPRc 模型和训练程序为创建新一代 QM/MM 势能提供了一种潜在的强大新工具,可应用于从药物发现到酶设计的广泛自由能应用。