Quantum‐Chemical Evaluation of the Interaction Between the <i>Mycobacterium tuberculosis</i> Dihydrofolate Reductase Enzyme With Classical and Potential Inhibitors

Tuberculosis (TB) remains a major global threat, demanding new therapeutic strategies. Dihydrofolate reductase (DHFR), essential for cell survival and a known drug target, has emerged as a promising enzyme for anti-TB drug development. Using crystallographic structures of Mycobacterium tuberculosis DHFR (MtDHFR) complexed with classical and potential inhibitors, a quantum-chemical analysis was performed through the molecular fractionation with conjugate caps (MFCC) scheme within the density functional theory (DFT) framework to quantify individual amino acid contributions to ligand-protein interactions. Energetically significant interactions were observed within a 6.0 Å pocket, when convergence of the total interaction energy (TIE) was found. The key residues I5, W6, D19, I20, R23, D27, Q28, H30, F31, R32, L50, K53, L57, R60, I94, and E111 were identified, along with the energetically relevant regions of the ligands and the major secondary structures of the protein. These results may guide the design of new anti-TB drugs.

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Publication Details

Journal
Chemistry & Biodiversity
Published
2026-04-01
DOI
https://doi.org/10.1002/cbdv.202502971
Primary Topic
Tuberculosis Research and Epidemiology
Type
article
Field-Weighted Citation Impact
0.00

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article

Quantum‐Chemical Evaluation of the Interaction Between the Mycobacterium tuberculosis Dihydrofolate Reductase Enzyme With Classical and Potential Inhibitors

V. N. Freire, U. L. Fulco, José Xavier Neto
Chemistry & Biodiversity
Tuberculosis Research and Epidemiology
article

Quantum‐Chemical Evaluation of the Interaction Between the Mycobacterium tuberculosis Dihydrofolate Reductase Enzyme With Classical and Potential Inhibitors

V. N. Freire, U. L. Fulco, José Xavier Neto
article en

Abstract

Tuberculosis (TB) remains a major global threat, demanding new therapeutic strategies. Dihydrofolate reductase (DHFR), essential for cell survival and a known drug target, has emerged as a promising enzyme for anti-TB drug development. Using crystallographic structures of Mycobacterium tuberculosis DHFR (MtDHFR) complexed with classical and potential inhibitors, a quantum-chemical analysis was performed through the molecular fractionation with conjugate caps (MFCC) scheme within the density functional theory (DFT) framework to quantify individual amino acid contributions to ligand-protein interactions. Energetically significant interactions were observed within a 6.0 Å pocket, when convergence of the total interaction energy (TIE) was found. The key residues I5, W6, D19, I20, R23, D27, Q28, H30, F31, R32, L50, K53, L57, R60, I94, and E111 were identified, along with the energetically relevant regions of the ligands and the major secondary structures of the protein. These results may guide the design of new anti-TB drugs.

Chemistry & BiodiversityVol. 23(4)
Universidade Federal do Ceará (BR), Universidade Federal do Rio Grande do Norte (BR)
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior, Conselho Nacional de Desenvolvimento Científico e Tecnológico
Good health and well-being
Openalex Percentile: Top 22%
Tuberculosis Research and Epidemiology
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