TY - JOUR
T1 - Pharmacophore-based virtual screening and molecular dynamics simulations for identifying potential enamine inhibitors of bacterial CTX-M-14 β-lactamases
AU - Haque, Shafiul
AU - Bantun, Farkad
AU - Jalal, Naif A.
AU - Faidah, Hani
AU - Babalghith, Ahmad O.
AU - Aldairi, Abdullah F.
AU - Rehman, Md Tabish
N1 - Publisher Copyright:
© 2025 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.
PY - 2025
Y1 - 2025
N2 - 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.
AB - 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.
KW - Antibacterial library
KW - CTX-M-14
KW - MD simulation
KW - docking
KW - virtual screening
UR - https://www.scopus.com/pages/publications/105017019036
U2 - 10.1080/16583655.2025.2557037
DO - 10.1080/16583655.2025.2557037
M3 - Artículo
AN - SCOPUS:105017019036
SN - 1658-3655
VL - 19
JO - Journal of Taibah University for Science
JF - Journal of Taibah University for Science
IS - 1
M1 - 2557037
ER -