Machine Learning-Guided Screening and Molecular Docking for Proposing Naturally Derived Drug Candidates Against MERS-CoV 3CL Protease.

Journal: International journal of molecular sciences
PMID:

Abstract

In this study, we utilized machine learning techniques to identify potential inhibitors of the MERS-CoV 3CL protease. Among the models evaluated, the Random Forest (RF) algorithm exhibited the highest predictive performance, achieving an accuracy of 0.97, an ROC-AUC score of 0.98, and an F1-score of 0.98. Following model validation, we applied it to a dataset of 14,194 naturally occurring compounds from PubChem. The top-ranked compounds were subsequently subjected to molecular docking, which identified Perenniporide B, Phellifuropyranone A, and Terrestrol G as the most promising candidates, with binding energies of -9.17, -9.08, and -8.71 kcal/mol, respectively. These compounds formed strong interactions with key catalytic residues, suggesting significant inhibitory potential against the viral protease. Furthermore, molecular dynamics simulations confirmed their stability within the active site, reinforcing their viability as antiviral agents. This study demonstrates the effectiveness of integrating machine learning with molecular modeling to accelerate the discovery of therapeutic candidates against emerging viral threats.

Authors

  • Mebarka Ouassaf
    Group of Computational and Medicinal Chemistry, LMCE Laboratory, University of Biskra, Biskra 07000, Algeria.
  • Radhia Mazri
    Group of Computational and Medicinal Chemistry, LMCE Laboratory, University of Biskra, Biskra 07000, Algeria.
  • Shafi Ullah Khan
    Inserm U1086 ANTICIPE (Interdisciplinary Research Unit for Cancer Prevention and Treatment), Normandie Univ, Université de Caen Normandie, 14076 Caen, France.
  • Kannan R R Rengasamy
    Laboratory of Natural Products and Medicinal Chemistry (LNPMC), Department of Pharmacology, Saveetha Dental College and Hospitals, Saveetha Institute of Medical and Technical Sciences (SIMATS), Thandalam, Chennai 602105, India.
  • Bader Y Alhatlani
    Unit of Scientific Research, Applied College, Qassim University, Buraydah 52571, Saudi Arabia.