- Drugs and Lactation Database (LactMed): Trimethoprim [BOOK]Drugs and Lactation Database (LactMed). National Library of Medicine (US): Bethesda (MD)BOOK
- Because of the low levels of trimethoprim in breastmilk, amounts ingested by the infant are small and would not be expected to cause any adverse effects in breastfed infants.
- Differentiation of the binding of two ligands to a tetrameric protein with a single symmetric active site by 19 F NMR. [Journal Article]
- R67 dihydrofolate reductase (R67 DHFR) is a plasmid-encoded enzyme that confers resistance to the antibacterial drug trimethoprim. R67 DHFR is a tetramer with a single active site that is unusual as both cofactor and substrate are recognized by symmetry-related residues. Such promiscuity has limited our previous efforts to differentiate ligand binding by NMR. To address this problem, we incorpora…
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- The structure and competitive substrate inhibition of dihydrofolate reductase from Enterococcus faecalis reveal restrictions to cofactor docking. [Journal Article]
- We are addressing bacterial resistance to antibiotics by repurposing a well-established classic antimicrobial target, the dihydrofolate reductase (DHFR) enzyme. In this work, we have focused on Enterococcus faecalis, a nosocomial pathogen that frequently harbors antibiotic resistance determinants leading to complicated and difficult-to-treat infections. An inhibitor series with a hydrophobic dihy…
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- Prevalence and antimicrobial susceptibilities of Vibrio, salmonella, and Aeromonas isolates from various uncooked seafoods in Thailand. [Journal Article]
- Uncooked seafood samples were collected from open markets and supermarkets in Bangkok, Thailand, and were examined for the presence of Vibrio, Salmonella, and Aeromonas species from January to February 2008. From 120 samples, 272 bacterial isolates were identified through biochemical testing. Of all sea bass, shrimp, oyster, and blood cockle samples (30 of each) that were processed for culture, 1…
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- NMR structures of apo L. casei dihydrofolate reductase and its complexes with trimethoprim and NADPH: contributions to positive cooperative binding from ligand-induced refolding, conformational changes, and interligand hydrophobic interactions. [Journal Article]
- In order to examine the origins of the large positive cooperativity (ΔG(0)(coop) = -2.9 kcal mol(-1)) of trimethoprim (TMP) binding to a bacterial dihydrofolate reductase (DHFR) in the presence of NADPH, we have determined and compared NMR solution structures of L. casei apo DHFR and its binary and ternary complexes with TMP and NADPH and made complementary thermodynamic measurements. The DHFR st…
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- Structural comparison of chromosomal and exogenous dihydrofolate reductase from Staphylococcus aureus in complex with the potent inhibitor trimethoprim. [Journal Article]
- Dihydrofolate reductase (DHFR) is the enzyme responsible for the NADPH-dependent reduction of 5,6-dihydrofolate to 5,6,7,8-tetrahydrofolate, an essential cofactor in the synthesis of purines, thymidylate, methionine, and other key metabolites. Because of its importance in multiple cellular functions, DHFR has been the subject of much research targeting the enzyme with anticancer, antibacterial, a…
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- Scope and limitations of the designer proline-rich antibacterial peptide dimer, A3-APO, alone or in synergy with conventional antibiotics. [Journal Article]
- The proline-rich antimicrobial peptide dimer, A3-APO, was designed based on a statistical analysis of native antibacterial peptide and protein sequences. Analysis of a series of structural analogs failed to identify any single or multiple amino acid modification or architectural changes that would significantly improve its potential as a clinical therapeutic. However, a single chain Chex1-Arg20 v…
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- Effects of co-operative ligand binding on protein amide NH hydrogen exchange. [Journal Article]
- Amide protection factors have been determined from NMR measurements of hydrogen/deuterium amide NH exchange rates measured on assigned signals from Lactobacillus casei apo-DHFR and its binary and ternary complexes with trimethoprim (TMP), folinic acid and coenzymes (NADPH/NADP(+)). The substantial sizes of the residue-specific DeltaH and TDeltaS values for the opening/closing events in NH exchang…
- Pharmacokinetics and bioavailability of trimethoprim-sulfamethoxazole in alpacas. [Journal Article]
- The pharmacokinetics and bioavailability of trimethoprim-sulfamethoxazole (TMP-SMX) were studied in six healthy male-castrate alpacas (Lama pacos) after intravenous (i.v.) or oral (p.o.) drug administration of 15 mg/kg TMP-SMX using a crossover design with a 2-week washout period. After 90 days one group (n = 3) was given a p.o. dose of 30 mg/kg TMP-SMX and the other group (n = 3) was given a p.o…
- Treatment of drug-induced toxic epidermal necrolysis (Lyell's syndrome) with intravenous human immunoglobulins. [Case Reports]
- Toxic epidermal necrolysis (TEN) is a rare drug-induced life-threatening disease. Currently, the disease is only treated by supportive and antiseptic measures. Quite recently intravenous immunoglobulins (IG) were shown to be a promising TEN treatment. The rationale for their use is based on the fact that keratinocyte apoptosis in TEN involves the CD95 (APO-1/Fas) cell surface receptor-ligand syst…
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- CHANGES IN URINARY ISOLATES AND THEIR ANTIBIOTIC RESISTANCE PATTERN. [Journal Article]
- A total of 338 urinary isolates were studied at AFMC, Pune during 1998 for species identification and antibiotic resistance. Out of 145 community isolates E coli were 67% followed by Staph aureus (11%). The hospital isolates of E coli and Proteus spp showed higher resistance to ampicillin (81% and 89% respectively) than to cefotaxime (23% and 22% respectively). K pneumoniae showed relatively high…
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- Structure and function of the dihydropteroate synthase from Staphylococcus aureus. [Journal Article]
- The gene encoding the dihydropteroate synthase of staphylococcus aureus has been cloned, sequenced and expressed in Escherichia coli. The protein has been purified for biochemical characterization and X-ray crystallographic studies. The enzyme is a dimer in solution, has a steady state kinetic mechanism that suggests random binding of the two substrates and half-site reactivity. The crystal struc…
- Circular dichroism studies of dihydrofolate reductase from a methotrexate-resistant strain of Escherichia coli B, MB 1428: ternary complexes. [Journal Article]
- Circular dichroism has been used to monitor the binding of pyridine nucleotide cofactors to enzyme-folate analog complexes of dihydrofolate reductase from Escherichia coli B (MB 1428). The enzyme binds one molar equivalent of many folate analogs and two molar equivalents of several pyridine nucleotide cofactors. The apo-enzyme has very low optical activity. The binding of folate analogs including…
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