A computational and machine learning approach to identify GPR40-targeting agonists for neurodegenerative disease treatment

PLoS One. 2024 Oct 8;19(10):e0306579. doi: 10.1371/journal.pone.0306579. eCollection 2024.

Abstract

The G protein-coupled receptor 40 (GPR40) is known to exert a significant influence on neurogenesis and neurodevelopment within the central nervous system of both humans and rodents. Research findings indicate that the activation of GPR40 by an agonist has been observed to promote the proliferation and viability of hypothalamus cells in the human body. The objective of the present study is to discover new agonist compounds for the GPR40 protein through the utilization of machine learning and pharmacophore-based screening techniques, in conjunction with other computational methodologies such as docking, molecular dynamics simulations, free energy calculations, and investigations of the free energy landscape. In the course of our investigation, we successfully identified five unreported agonist compounds that exhibit robust docking score, displayed stability in ligand RMSD and consistent hydrogen bonding with the receptor in the MD trajectories. Free energy calculations were observed to be higher than control molecule. The measured binding affinities of compounds namely 1, 3, 4, 6 and 10 were -13.9, -13.5, -13.4, -12.9, and -12.1 Kcal/mol, respectively. The identified molecular agonist that has been found can be assessed in terms of its therapeutic efficacy in the treatment of neurological diseases.

MeSH terms

  • Humans
  • Ligands
  • Machine Learning*
  • Molecular Docking Simulation*
  • Molecular Dynamics Simulation*
  • Neurodegenerative Diseases* / drug therapy
  • Neurodegenerative Diseases* / metabolism
  • Protein Binding
  • Receptors, G-Protein-Coupled* / agonists
  • Receptors, G-Protein-Coupled* / metabolism
  • Thermodynamics

Substances

  • Receptors, G-Protein-Coupled
  • FFAR1 protein, human
  • Ligands

Grants and funding

This research has been funded by King Salman Center for Disability Research through Research Group No. KSRG-2022-086. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.