Integrated Computational Omics Approach to Identify Novel Natural Product Inhibitors Targeting KIF11 in Endometrial

Shazma Sarwat1, Koel Mukherjee1

  • 1Department of Bioengineering and Biotechnology, Birla Institute of Technology Mesra, Ranchi, Jharkhand, India.

Insights

This study identified glycocholic acid (GCA) as a promising natural compound to target Kinesin Family Member 11 (KIF11) in endometrial carcinoma (EC). GCA shows superior stability for developing new precision therapeutics against EC.

Area of Science:

  • Oncology
  • Pharmacology
  • Computational Biology

Background:

  • Endometrial carcinoma (EC) is a heterogeneous cancer with Kinesin Family Member 11 (KIF11) overexpression.
  • There is a need for targeted therapies against KIF11 in EC.

Purpose of the Study:

  • To identify natural product-based KIF11 inhibitors for EC treatment.
  • To leverage multiomics and structural bioinformatics for drug discovery.

Main Methods:

  • Integrated computational framework: multiomics analysis (TCGA, CPTAC) and structural bioinformatics.
  • Pharmacophore-based virtual screening of ~400,000 natural compounds against KIF11 active site (PDB ID: 2X7C).
  • ADMET profiling, molecular docking, and 100 ns molecular dynamics simulations.

Main Results:

  • KIF11 was significantly upregulated in EC at transcriptomic and proteomic levels.
  • Glycocholic acid (GCA) demonstrated superior conformational stability and persistent hydrogen bonding compared to glycodeoxycholic acid (GDCA).
  • GCA showed a stable RMSD profile (~1.5 Å) and key interactions with KIF11 residues LYS111 and GLU118.

Conclusions:

  • Glycocholic acid (GCA) is a robust lead candidate for targeted EC therapy.
  • Integrating transcriptomic, proteomic, and structural data is effective for precision therapeutics development.
  • This approach can accelerate the discovery of novel natural product-based drugs for endometrial carcinoma.