Integrated Computational Omics Approach to Identify Novel Natural Product Inhibitors Targeting KIF11 in Endometrial Carcinoma
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Published on: May 27, 2021
Shazma Sarwat1, Koel Mukherjee1
1Department of Bioengineering and Biotechnology, Birla Institute of Technology Mesra, Ranchi, Jharkhand, India.
Abstract:
Endometrial carcinoma (EC) presents a growing global health challenge, characterized by significant molecular heterogeneity and the overexpression of the mitotic motor protein Kinesin Family Member 11 (KIF11). To address the critical need for targeted therapeutics, this study employed an integrated computational framework combining multiomics expression analysis with structural bioinformatics to identify novel natural product-based inhibitors. Validation using TCGA and CPTAC datasets confirmed significant upregulation of KIF11 in EC at both transcriptomic and proteomic levels. A pharmacophore-based virtual screening of approximately 400,000 natural compounds was conducted against the KIF11 active site (PDB ID: 2X7C), followed by ADMET profiling and molecular docking. While glycodeoxycholic acid (GDCA) exhibited the highest docking affinity (-9.5 kcal/mol), subsequent 100 ns molecular dynamics simulations revealed that glycocholic acid (GCA) possessed superior conformational stability. GCA demonstrated a stable RMSD profile (approximately 1.5 Å) and persistent hydrogen bonding with key residues LYS111 and GLU118, unlike the fluctuating profile observed in GDCA. This study identifies GCA as a robust lead candidate, underscoring the efficacy of integrating transcriptomic and proteomic data with structural biology to drive precision therapeutics for EC.
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.
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