Multi-regulator of EZH2-PPARs Therapeutic Targets: A Hallmark for Prospective Restoration of Pancreatic Insulin Production and Cancer Dysregulation

Appl Biochem Biotechnol. 2023 Dec;195(12):7520-7552. doi: 10.1007/s12010-023-04433-w. Epub 2023 Apr 3.

Abstract

The unexpected rise in cancer and diabetes statistics has been a significant global threat, inciting ongoing research into various biomarkers that can act as innovative therapeutic targets for their management. The recent discovery of how EZH2-PPARs' regulatory function affects the metabolic and signalling pathways contributing to this disease has posed a significant breakthrough, with the synergistic combination of inhibitors like GSK-126 and bezafibrate for treating these diseases. Nonetheless, no findings on other protein biomarkers involved in the associated side effects have been reported. As a result of this virtual study, we identified the gene-disease association, protein interaction networks between EZH2-PPARs and other protein biomarkers regulating pancreatic cancer and diabetes pathology, ADME/Toxicity profiling, docking simulation and density functional theory of some natural products. The results indicated a correlation between obesity and hypertensive disease for the investigated biomarkers. At the same time, the predicted protein network validates the link to cancer and diabetes, and nine natural products were screened to have versatile binding capacity against the targets. Among all natural products, phytocassane A outperforms the standard drugs' (GSK-126 and bezafibrate) in silico validation for drug-likeness profiles. Hence, these natural products were conclusively proposed for additional experimental screening to complement the results on their utility in drug development for diabetes and cancer therapy against the EZH2-PPARs' new target.

Keywords: Diabetes mellitus; EZH2-PPARs; In silico profiling; Natural products; Pancreatic cancer; Protein–protein network.

MeSH terms

  • Bezafibrate
  • Biological Products* / pharmacology
  • Biomarkers
  • Diabetes Mellitus* / drug therapy
  • Diabetes Mellitus* / genetics
  • Enhancer of Zeste Homolog 2 Protein / genetics
  • Humans
  • Insulin
  • Molecular Docking Simulation
  • Neoplasms* / drug therapy
  • Neoplasms* / genetics
  • Peroxisome Proliferator-Activated Receptors
  • Prospective Studies

Substances

  • Insulin
  • Peroxisome Proliferator-Activated Receptors
  • Bezafibrate
  • Biological Products
  • Biomarkers
  • EZH2 protein, human
  • Enhancer of Zeste Homolog 2 Protein