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At least 1,315 records · Page 73Linked to original sources
PubMed1973

The interaction of elongation factor G with N-acetylphenylalanyl transfer RNA-ribosome complexes.

N-Acetyl-Phe-tRNA, nonenzymically bound to the acceptor site of Escherichia coli ribosomes, readily undergoes translocation in the presence of elongation factor (EF)-G and GTP. The translocated N-acetyl-Phe-tRNA, bound to the ribosomal donor site, prevents further interaction of EF-G with the ribosome, for it inhibits the GTP hydrolysis that takes place in the presence of EF-G and ribosomes and it decreases the formation of either the GDP.EF-G.fusidic acid.ribosome complex or the 5'-guanylylmethylenediphosphonate.EF-G.ribosome complex. Deacylation with puromycin of the donor site-bound N-acetyl-Phe-tRNA reverses these inhibitions, even though the tRNA(Phe) moiety remains bound to the ribosme. These results suggest that ribosomes complexed with messenger RNA and peptidyl-tRNA may be restricted in their ability to interact with EF-G to that part of the elongation cycle when peptidyl-tRNA is in the acceptor site, and deacylated tRNA in the donor site. Deacylation of the donor site-bound peptidyl-tRNA associated with peptide bond formation may control the interaction of EF-G with the ribosome.

Binding Sites↗
PubMed1973

Synthesis of stable RNA in stringent Escherichia coli cells in the absence of charged transfer RNA.

It has been possible to demonstrate the complete absence of either charged tRNA(Glu) or charged tRNA(Val) at 42 degrees by the use of two stringent strains of E. coli, one temperature-sensitive for glutamyl-tRNA synthetase and the other temperature-sensitive for valyl-tRNA synthetase. In both strains, stable RNA synthesis ceases, and guanosine tetraphosphate accumulates upon incubation at the nonpermissive temperature. Unique among a series of antibiotics tested, only tetracycline was able to stimulate stable RNA synthesis and to cause disappearance of the guanosine nucleotide. In this regard tetracycline and the "relaxed" gene product appear to be analogous.

Amino Acyl-tRNA Synthetases↗
PubMed1976

A ribosome-dependent GTPase from yeast distinct from elongation factor 2.

Three proteins required for poly(U)-directed polyphenylalanine synthesis have been separated from yeast. Two of the factors correspond to the elongation factors 1 and 2 described for other eukaryotic systems, according to the criteria of phenylalanyl-tRNA binding and diphtheria toxin-catalyzed ADP-ribosylation. The third protein, while absolutely required for polyphenylalanine synthesis, was a more active ribosome-dependent GTPase than elongation factor 2.

Adenosine Diphosphate↗
PubMed1976

Transcription-translation and translation-messenger RNA decay coupling: separate mechanisms for different messengers.

Antibiotics were used to inhibit protein synthesis at specific steps in the biosynthetic pathway. In this way, it was possible to study the coupling of protein synthesis to the accumulation of biologically active mRNA in T4-infected Escherichia coli. Functional mRNA for the phage enzymes deoxynucleotide kinase (EC 2.7.4.4; ATP: nucleoside monophosphate phosphotransferase or nucleosidemonophosphate kinase) and alpha-glucosyltransferase (EC 2.4.1.5; 1, 4-alpha-D-glucan: 1, 6-alpha-D-glucan 6-alpha-glucosyltransferase or dextrin dextranase) accumulated during inhibition of protein synthesis irrespective of the step in the synthesis of protein that was blocked. Under these conditions, however, the rate of mRNA synthesis for both enzymes was significantly inhibited. In contrast, the rate of degradation of these mRNAs was markedly dependent on the step in protein synthesis that was inhibited. That is, the site for mRNase action was different for each message. The most important step in protein synthesis required for the stability of deoxynucleotide kinase mRNA is the initiation step. A single ribosome bound to the 5' end of the deoxynucleotide kinase mRNA can stabilize the molecule. On the other hand, the initiation event does not seem to be important for stabilizing the alpha-glucosyltransferase mRNA. Instead, a high ribosome denisty on the alpha-glucosyltransferase messenger is required to achieve significant stability. Therefore, in studying messenger metabolism, it is important to focus on the functional stability of specific mRNAs instead of on total messenger since each mRNA can be metabolized differently.

Anti-Bacterial Agents↗
PubMed1973

Recognition of streptococcal DNA by a mutant pneumococcus unable to discriminate among markers in pneumococcal DNA.

A mutant strain of pneumococcus which fails to discriminate against low-efficiency markers during transformation by homospecific pneumococcal donor DNA retains the wild-type capacity to discriminate against heterospecific (streptococcal) donor DNA. We conclude that discrimination against heterospecific DNA must differ from that against low-efficiency markers by the kind or number of elements being recognized.

DNA, Bacterial↗
PubMed1981

Antistaphylococcal activity of rifampin with other antibiotics.

The bactericidal activity of rifampin plus other antibiotics was examined with in vitro checkerboard dilutions against 15 strains of staphylococci, with time-kill studies, and with determinations of serum bactericidal activities (SBAs) in volunteers. In vitro synergism was found consistently only in inhibitory assays with rifampin plus minocycline. Time-kill studies with rifampin plus methicillin revealed enhanced killing at concentrations close to the MBC but reduced combined activity at higher concentrations. SBAs with rifampin, oxacillin, and the two drugs in combination were studied in three treatment regimens (regimen A: 2 g of oxacillin and 300 mg of rifampin; regimen B: 1 g of oxacillin and 450 mg of rifampin; and regimen C: 3 g of oxacillin and 450 mg of rifampin). The SBA against methicillin-sensitive Staphylococcus aureus was significantly lower with the two drugs in combination than with oxacillin alone in regimen A but not in regimen B. In vitro synergy with rifampin plus other antibiotics was not frequent. At high concentrations, the bactericidal activity of oxacillin was reduced by rifampin, but killing activity may be enhanced at low concentrations of oxacillin.

Anti-Bacterial Agents↗
PubMed1987

In-vitro susceptibility of gram-positive cocci to LY146032 teicoplanin, sodium fusidate, vancomycin, and rifampicin.

LY146032, a new antimicrobial agent with activity against Gram-positive cocci, was tested against methicillin-susceptible and methicillin-resistant Staphylococcus aureus, methicillin-susceptible and methicillin-resistant Staph. epidermidis, Staph. saprophyticus, and Streptococcus faecalis. MIC90s in cation-supplemented Mueller Hinton broth by the microdilution broth method were less than 1.0 mg/l for all organisms tested. Increasing or decreasing the inoculum size did not appreciably effect the MIC50 or MIC90 for any organism group nor did decreasing the incubation temperature. The addition of sodium chloride to the test system did not appreciably effect the susceptibility of methicillin-resistant Staph. aureus to LY146032. All organisms were 4 to 32 times more susceptible to LY146032 than to vancomycin. The Staph. aureus had LY146032 susceptibility patterns which were similar to those of teicoplanin and sodium fusidate. LY146032 was 4-16 times more active than teicoplanin against Staph. saprophyticus and Staph. epidermidis while teicoplanin was 8-16 times more active than LY146032 against Str. faecalis.

Anti-Bacterial Agents↗
PubMed1989

Pharmacokinetics and tolerance of a new film-coated tablet of sodium fusidate administered as a single oral dose to healthy volunteers.

Single oral doses of 250, 500, 750 and 1000 mg of sodium fusidate as one, two, three and four film-coated 250 mg tablets were compared in a cross over design trial with a solution dose of 500 mg in 12 healthy male volunteers. The effect of food on absorption of two-film coated tablets was also studied. Compared with the dose given as a solution, tablets gave complete oral absorption, the area under the curve (AUC) for blood concentration being virtually identical. After administration of 250, 500, 750 and 1000 mg the mean of the maximum serum concentrations (Cmax) was 11.6 +/- 1.1, 30.6 +/- 2.2, 48.1 +/- 3.0 and 65.2 +/- 4.2 mg/l, respectively, indicating a greater than expected increase in Cmax with increasing dose. This was also apparent with AUC, while there was a significant trend for beta, the terminal slope of the serum/concentration time curve, to decrease. Food significantly reduced Cmax and delayed Tmax but did not affect AUC or beta. Dosage had no effect on parameters of renal, hepatic or haemopoietic function but 25% of the volunteers complained of upper gastro-intestinal symptoms mainly at the highest dose studied.

Administration, Oral↗
PubMed1990

Pharmacokinetics of sodium fusidate after single and repeated infusions and oral administration of a new formulation.

The pharmacokinetics of sodium fusidate were studied in eight healthy volunteers (five males and three females) aged 21 to 33 years (29.1 +/- 1.5), weight 46 to 79 kg (61.6 +/- 4.0 kg). First, the subjects were given 500 mg of sodium fusidate by infusion over two hours; secondly, one month later, the volunteers were given 500 mg of fusidate by infusion every eight hours for three days; thirdly, two 250 mg tablets of a new film coated formulation were administered as a single dose. Plasma concentrations of fusidate were measured by HPLC. Peak plasma concentrations reached at the end of the first and the last infusions were 52 +/- 5 mg/l and 123 +/- 12 mg/l respectively. The following mean pharmacokinetic parameters were obtained after single intravenous administration: elimination half-life 10 +/- 1 h, total clearance 22 +/- 2 ml/min and volume of distribution 0.30 +/- 0.04 l/kg. After repeated administration the half-life and the volume of distribution remained unchanged whereas total clearance was halved (11 +/- 1 ml/min). This leads to an experimental accumulation ratio (3.6 +/- 0.2) higher than the theoretical one (1.8 +/- 0.1; P less than 0.01). Consequently, mean trough and peak steady state plasma concentrations (81 +/- 9 and 123 +/- 12 mg/l respectively) are higher than those expected from the single dose kinetics (33 +/- 4 and 76 +/- 7 mg/l respectively). This dose regimen leads to concentrations well above the MIC for most sensitive strains.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Oral↗
PubMed1996

Treatment of endocarditis with teicoplanin: a retrospective analysis of 104 cases.

Infective endocarditis is an uncommon disease but retains a high mortality. Glycopeptides are used for patients with resistant pathogens, those allergic to penicillins or for those outside the hospital. The once daily administration of teicoplanin and its low toxicity suggest that it would be suitable for use in the long courses required for endocarditis. However, the dosage and combinations to be used require further study. A retrospective review has been made of 104 episodes of endocarditis treated with teicoplanin in 101 patients seen over 7 years. Most patients had been referred to major London hospitals following failure of medical treatment. After three loading doses of 400 mg, teicoplanin was given at a dose of 400 mg/day in combination with other antibiotics such as gentamicin. Follow up was for one year. The most common pathogens were Streptococcus sanguis (15 cases), Staphylococcus aureus (13 cases) and Staphylococcus epidermidis (10 cases). Of 80 patients febrile at the start of treatment with teicoplanin, 63 (79%) lost their fever within a median of 2 days (1-35 days). Cure without surgery was effected in 50 (48%) and 75% of patients survived. Other antibiotics, usually gentamicin or rifampicin, were used in 92 (90%) of patients. Two strains of Streptococcus spp. were said to be resistant but there was no relationship between MIC of teicoplanin and outcome. Pathogens with a high MBC tended to be more likely to resist treatment. Adverse effects resulted in the withdrawal of teicoplanin in 20 cases (19%) but most events were mild and renal deterioration occurred in only five patients. Teicoplanin was effective in the treatment of endocarditis and appeared to be safe given the severity of disease in the patients treated.

Adult↗