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 original | Inglés |
|---|---|
| Número de artículo | 2557037 |
| Publicación | Journal of Taibah University for Science |
| Volumen | 19 |
| N.º | 1 |
| DOI | |
| Estado | Publicada - 2025 |
ODS de las Naciones Unidas
Este resultado contribuye a los siguientes Objetivos de Desarrollo Sostenible
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ODS 3: Salud y bienestar
Huella
Profundice en los temas de investigación de 'Pharmacophore-based virtual screening and molecular dynamics simulations for identifying potential enamine inhibitors of bacterial CTX-M-14 β-lactamases'. En conjunto forman una huella única.Citar esto
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