Comparison of the binding of trimethoprim and trimethoprim analogues to bacterial dihydrofolate reductase
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منابع مشابه
Isolation and characterization of dihydrofolate reductase from trimethoprim-susceptible and trimethoprim-resistant Pseudomonas cepacia.
Trimethoprim resistance was investigated in cystic fibrosis isolates of Pseudomonas cepacia. Determination of the MIC of trimethoprim for 111 strains revealed at least two populations of resistant organisms, suggesting the presence of more than one mechanism of resistance. Investigation of the antibiotic target, dihydrofolate reductase, was undertaken in both a susceptible strain and a strain w...
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Previous crystallographic studies of the antibacterial trimethoprim in complexes with bacterial and avian dihydrofolate reductases have shown substantial differences in the mode of binding, providing plausible explanations for the origin of the remarkable species selectivity of this inhibitor (Matthews, D. A., Bolin, J. T., Burridge, J. M., Filman, D. J., Volz, K. W., Kaufman, B. T., Beddell, C...
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The machine learning program GOLEM from the field of inductive logic programming was applied to the drug design problem of modeling structure-activity relationships. The training data for the program were 44 trimethoprim analogues and their observed inhibition of Escherichia coli dihydrofolate reductase. A further 11 compounds were used as unseen test data. GOLEM obtained rules that were statis...
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NMR measurements have been used to investigate rates of ring-flipping and the activation parameters for the trimethoxybenzyl ring of the antibacterial drug trimethoprim (TMP) bound to Lactobacillus casei dihydrofolate reductase (DHFR) for a series of ternary complexes formed with analogues of the coenzyme NADPH. Rates were obtained at several temperatures from line shape analyses ((13)C-edited ...
متن کاملRole of the dihydrofolate reductase DfrA (Rv2763c) in trimethoprim-sulfamethoxazole (co-trimoxazole) resistance in Mycobacterium tuberculosis.
We thank Wang et al. for clarifying the role of the dihydrofolate reductase DfrA (Rv2763c) in isoniazid (INH) resistance (16). Concerning potential candidates for the unknown INH resistance mechanism(s), we would like to point out that the aldC (Rv2858c) T21A mutation is also present in Mycobacterium tuberculosis strains C (GenBank accession no. AAKR00000000) and CDC1551 (7), both of which belo...
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ژورنال
عنوان ژورنال: Acta Crystallographica Section A Foundations of Crystallography
سال: 1981
ISSN: 0108-7673
DOI: 10.1107/s010876738109781x