Center for Computational Natural Sciences and Bioinformatics, International Institute of Information Technology, Hyderabad 500 032, India.
École Centrale School of Engineering, Mahindra University, Hyderabad 500 043, India.
J Chem Inf Model. 2021 Dec 27;61(12):5815-5826. doi: 10.1021/acs.jcim.1c01341. Epub 2021 Dec 6.
The design of new inhibitors for novel targets is a very important problem especially in the current scenario with the world being plagued by COVID-19. Conventional approaches such as high-throughput virtual screening require extensive combing through existing data sets in the hope of finding possible matches. In this study, we propose a computational strategy for de novo generation of molecules with high binding affinities to the specified target and other desirable properties for druglike molecules using reinforcement learning. A deep generative model built using a stack-augmented recurrent neural network initially trained to generate druglike molecules is optimized using reinforcement learning to start generating molecules with desirable properties like LogP, quantitative estimate of drug likeliness, topological polar surface area, and hydration free energy along with the binding affinity. For multiobjective optimization, we have devised a novel strategy in which the property being used to calculate the reward is changed periodically. In comparison to the conventional approach of taking a weighted sum of all rewards, this strategy shows an enhanced ability to generate a significantly higher number of molecules with desirable properties.
针对新型靶点设计新的抑制剂是一个非常重要的问题,尤其是在当前全球受到 COVID-19 困扰的情况下。传统方法,如高通量虚拟筛选,需要广泛梳理现有的数据集,以期找到可能的匹配。在这项研究中,我们提出了一种使用强化学习从头生成与指定靶标具有高结合亲和力和其他理想药物特性的分子的计算策略。使用堆栈增强递归神经网络构建的深度生成模型最初经过训练可生成类药物分子,然后使用强化学习对其进行优化,开始生成具有理想特性的分子,如 LogP、药物相似性的定量估计、拓扑极性表面积和水合自由能以及结合亲和力。对于多目标优化,我们设计了一种新颖的策略,其中用于计算奖励的属性会定期更改。与传统的计算所有奖励的加权和的方法相比,这种策略显示出了生成具有理想特性的分子数量显著增加的能力。