Combined usage of ligand- and structure-based virtual screening in the artificial intelligence era.

Journal: European journal of medicinal chemistry
PMID:

Abstract

Drug design has always been pursuing techniques with time- and cost-benefits. Virtual screening, generally classified as ligand-based (LBVS) and structure-based (SBVS) approaches, could identify active compounds in the large chemical library to reduce time and cost. Owing to the intrinsic flaws and complementary nature of both approaches, continued efforts have been made to combine them to mitigate limitations. Meanwhile, the emergence of machine learning (ML) endows them with opportunities to leverage vast amounts of data to improve their defects. However, few discussions on how to merge ML-improved LBVS and SBVS have been conducted. Therefore, this review provides insights into combined usage of ML-improved LBVS and SBVS to enlighten medicinal chemists to utilize these joint strategies to lift the screening efficiency as well as AI professionals to design novel techniques.

Authors

  • Jingyi Dai
    School of Stomatology, Hainan Medical University, Haikou 570100, China.
  • Ziyi Zhou
    Department of Otolaryngology Head and Neck Surgery,the Second Xiangya Hospital,Central South University,Changsha,410011,China.
  • Yanru Zhao
    School of Intelligent Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, Sichuan, China. Electronic address: zhaoyanru086@gmail.com.
  • Fanjing Kong
    School of Intelligent Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, Sichuan, China. Electronic address: kongfanjing927@126.com.
  • Zhenwei Zhai
    School of Intelligent Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, China.
  • Zhishan Zhu
    School of Intelligent Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, Sichuan, China. Electronic address: zhishan0529@163.com.
  • Jie Cai
    Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-Sen University, 132 East Circle at University City, Guangzhou, 510006, China.
  • Sha Huang
    School of Intelligent Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, Sichuan, China. Electronic address: huangsha1pot26@126.com.
  • Ying Xu
    School of Biological and Food Engineering Changzhou University Changzhou Jiangsu China.
  • Tao Sun
    Janssen Research & Development, LLC, Raritan, NJ, USA.