Pharmacophore-based virtual screening and molecular dynamics simulations for identifying potential enamine inhibitors of bacterial CTX-M-14 β-lactamases

  • Shafiul Haque
  • , Farkad Bantun
  • , Naif A. Jalal
  • , Hani Faidah
  • , Ahmad O. Babalghith
  • , Abdullah F. Aldairi
  • , Md Tabish Rehman

Producción científica: Contribución a una revistaArtículorevisión exhaustiva

Resumen

CTX-M-14 β-lactamase is a key enzyme linked to antibiotic resistance, making it a critical target in infectious disease research. Here, a pharmacophore model based on known inhibitor interactions was used to virtually screen the Enamine antibacterial library. Top hits were docked into the CTX-M-14 active site using Glide, and filtered based on docking score, interaction quality, and ADMET properties. Lead compound E10 showed strong binding (GlideScore = −8.7 kcal/mol), excellent predicted oral absorption, low metabolic risk, and non-toxic excretion. Simulation studies showed that the CTX-M-14 and E10 complex remained stable. RMSF analysis indicated minimal fluctuations for most residues. E10 formed extensive hydrogen bonds with key active-site residues, providing strong polar stabilization. Cross-correlation analysis indicated cooperative residue dynamics were preserved. MM/GBSA calculations yielded a ΔG_bind of −58.89 kcal/mol, driven by favourable van der Waals and electrostatic interactions. These findings support E10 as a stable, high-affinity CTX-M-14 inhibitor suitable for further development.

Idioma originalInglés
Número de artículo2557037
PublicaciónJournal of Taibah University for Science
Volumen19
N.º1
DOI
EstadoPublicada - 2025

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