Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: CAS:107-95-9 (beta-alanine)
 2,037 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Two linear peptides, D-leucyl-L-prolyl-L-isoleucyl-L-valyl-L-alanyl-beta-alanine (I) and D-leucyl-L-prolyl-L-isoleucyl-L-valyl-N-methyl-L-alanyl-beta-alanine (II), whose sequences were designed from protodestruxin and desmethyldestruxin B by replacing D-leucic acid with D-leucine, two cyclic hexadepsipeptides with insecticidal and immunodepressant activities, have been found to be cyclized in unusually high yields (>85%). In order to gain insight into the conformation and the relative flexibility of different constituent residues in these linear peptides, we have applied various techniques of 2D-NMR spectroscopy coupled with dynamic simulated annealing by computer modeling to establish the solution conformations of these two linear peptides. Based on the derived structures, it is found that the distances between N- and C-terminal residues of both peptides are short enough to facilitate the cyclization, thus collaborating the observation of favorable cyclization yields for both linear peptides.
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PMID:Conformational study of two linear hexapeptides by two-dimensional NMR and computer-simulated modeling: implication for peptide cyclization in solution. 860 29

The composition of 36 amino acids and related amino compounds is presented for plasma, aorta, heart, pancreas, and bronchi. The distribution pattern of these biochemicals is similar but not identical among the tissues. The effect of an acute dose of ethanol (2 g/kg, i.p.) on these amino acids and related compounds was then studied. In the plasma, alanine, arginine, aspartic acid, beta-alanine, glycine, phenylalanine, and serine are decreased. In the aorta, ammonia and taurine are decreased. In the heart, aspartic acid and leucine are decreased, and carnosine, GABA, glutamic acid, and ornithine are increased. In the pancreas, asparagine and taurine are decreased, and citrulline, cysteine, histidine, and isoleucine are increased. In the bronchi, GABA, ethanolamine, histidine, taurine, and isoleucine are decreased. A number of correlations of some compounds in plasma or tissues were found but differed often between control and ethanol-treated animals. Ethanol-induced tissue changes generally do not correlate with plasma changes and are mostly specific for a given tissue.
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PMID:Effect of ethanol on amino acids and related compounds in rat plasma, heart, aorta, bronchus, and pancreas. 881 52

Previous studies showed that the in situ absorption of baclofen in rat jejunum was inhibited by beta-alanine, a nonessential amino acid, and therefore mediated, at least in part, by some beta-amino acid carrier. In this paper a similar study was undertaken using taurine, a sulfonic beta-amino acid, in order to evaluate its effect and to establish a general inhibition model. To achieve this goal, remaining concentrations of inhibitor were also measured and incorporated into the model. Previously, kinetic absorption in situ parameters for taurine in free solution were obtained: Vm = 27.73 +/- 9.99 mM h-1, K(m) = 8.06 +/- 2.82 mM, Ka (passive difussion component) = 0.40 +/- 0.28 h-1. Isotonic solutions containing 0.5 mM baclofen with starting taurine concentrations ranging from 0 to 100 mM were perfused in rat jejunum, and the remaining concentrations of both compounds were measured. The apparent rate pseudoconstant of the drug clearly decreased as the remaining taurine concentration increased. The interaction can be described as a complete competitive inhibition plus a second component, K, noninhibited, K = 0.58 (+/- 0.03) h-1, Ki = 20.62 (+/- 4.04) mM, Vmi = 28.12 (+/- 6.12) mM h-1, Kmi = 11.71 (+/- 2.53) mM, Kai = 0.47 (+/- 0.10) h-1. A residual absorption of baclofen in the presence of high taurine concentrations was observed, which should be attributed to another transport system not associated with the taurine carrier. In order to elucidate whether or not taurine and beta-alanine carriers are two separate entities that baclofen can use for absorption, further experiments using beta-alanine and taurine together as inhibitors (baclofen, 0.5 mM; beta-alanine, 50 mM, and taurine, 50 mM) were developed. Results indicated that baclofen and both amino acids share the same carrier in the intestinal absorption process. We have completed studies using leucine, taurine, and GABA together as inhibitors of drug absorption. An isotonic perfusion solution of 0.5 mM baclofen in the presence of 50 mM leucine, 25 mM taurine, and 25 mM GABA was perfused. Under these conditions the absorption rate pseudoconstant of baclofen decreases until 0.080 h-1 (+/- 0.069). Practical implications of these phenomena are briefly discussed.
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PMID:Interaction of taurine on baclofen intestinal absorption: a nonlinear mathematical treatment using differential equations to describe kinetic inhibition models. 892 34

Methylmercury cysteine (MeHg-cysteine) uptake by rat erythrocytes (RBC) was undertaken at 5 and 20 degrees C. The effects of several amino acids, their derivatives, ATP, Na+, Mg2+ and membrane potential on MeHg-cysteine uptake were examined. The results showed that MeHg-cysteine uptake was temperature-dependent, Na(+)-dependent at 20 degrees C, partly Na(+)-dependent at 5 degrees C and Mg(2+)-dependent at 5 and 20 degrees C. The membrane potential had a very slight effect on MeHg-cysteine uptake. N-Acetyl-L-cysteine (AC), alanine, beta-alanine, cysteine sulphinic acid (CSA), gamma-aminobutyric acid (GABA), D-phenylalanine, phenylalanine, serine and taurine inhibited MeHg-cysteine uptake at 5 degrees C. Tryptophan both stimulated and inhibited at different sampling times at 5 degrees C. Glycine and methionine had stimulation at 5 degrees C. Aspartic acid, isoleucine, leucine and tyrosine had no effect on MeHg-cysteine uptake. GABA, D-phenylalanine and tryptophan lost their effects at 20 degrees C. The effects of glycine and serine had reversed at 20 degrees C. The half-time of MeHg-cysteine uptake was ca. 0.57 h at 5 degrees C and 0.23 h at 20 degrees C. Several amino acids and their derivatives had an influence on the half-times of MeHg-cysteine uptake. The present study suggested that MeHg-cysteine uptake by rat RBC at lower temperature involved several overlapping transport systems; the greatest contribution was likely to be due to system ASC. Direct evidence for system L in MeHg-cysteine uptake was not obtained in the present study.
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PMID:Uptake of methylmercury cysteine by rat erythrocytes at lower temperature. 893 81

The role of sodium in transport of bipolar and cationic amino acids and their interactions were examined in vitro by measuring unidirectional influx across the brush-border membrane of intact rat jejunal and rabbit ileal epithelia. The chloride-dependent and beta-alanine inhibitable B(0,+) present in rabbit ileum was blocked by combining inhibition by beta-alanine with Na(+)- or Cl(-)-free conditions. Under these conditions, lysine influx across the brush-border membrane is Na+ independent. All Na+-independent influx of cationic and bipolar amino acids is by a system b(0,+) equivalent in the brush-border membrane of both species, where a system y+ is not present. System b(0,+) is shown to be a potent exchanger of intracellular leucine for extracellular lysine and of intracellular lysine for extracellular leucine. The model used to explain leucine stimulation of mucosa to serosa lysine transport can explain Na+ dependence of net lysine absorption. On the assumption that b(0,+) in situ, like the transporter induced by retroperitoneal brown adipose tissue in Xenopus laevi oocytes, acts as an obligatory exchanger, this model can also explain the effects of lysine on short-circuit current and net transport of sodium and the effect on transport capacity by preincubation at Na+-free conditions.
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PMID:Na+-independent transport of bipolar and cationic amino acids across the luminal membrane of the small intestine. 914 2

The mechanisms of carrier-mediated transport of gamma-aminobutyric acid (GABA) at the blood-brain barrier (BBB) were examined by investigating [3H]GABA uptake by isolated bovine brain capillaries, monolayers of primary cultured brain capillary endothelial cells (BCECs) attached to plates or suspended BCECs. The uptake of [3H]GABA was concentration-dependent and saturable. Nonlinear regression analysis of the original data indicated the existence of two distinct high and low-affinity GABA transporters on isolated brain capillaries or suspended BCECs, with Km1, Km2, Vm1 and Vm2 equal to 25.3 microM, 485.2 microM, 3.6 and 8.4 nmol/5 min/mg protein, respectively, for the capillaries, and 21.3 microM, 322.0 microM, 6.1 and 15.7 nmol/5 min/mg protein, respectively, for the suspended BCECs. In contrast, a single low-affinity transporter was found for monolayers of BCECs attached to plates with Km and Vm equal to 338.7 microM and 18.8 nmol/5 min/mg protein, respectively. Subcellular location of the two distinct transporters on BCECs is discussed, suggesting that the low-affinity GABA transporter is probably localized to the luminal membrane of BCECs, and the high-affinity GABA transporter is probably localized to the antiluminal membrane. Low temperature (4 degreesC) and metabolic inhibitors markedly diminished both high and low-affinity uptakes of [3H]GABA by isolated brain capillaries. The substitution of Na+ with choline+, K+ or Li+ with the counter anion Cl- almost completely abolished both uptakes. Substitution of Cl- with Br-, I-, F- or NO3- in the presence of Na+ significantly reduced both uptakes to different extents. Alanine, leucine, phenylalanine, arginine, glutamate and pyruvate had no obvious effect on either uptake. Probenecid, amino-oxyacetic acid, beta-alanine, taurine, betaine, and nipecotic acid significantly reduced both uptakes. These data suggested that both the GABA transporters at the BBB were temperature, metabolic energy, Na+ and Cl--dependent, and may be specific and different from the known monocarboxylic acid, GABA and other amino acid transporters, which may play a role in the disposition of GABA in the brain.
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PMID:Sodium and chloride-dependent high and low-affinity uptakes of GABA by brain capillary endothelial cells. 979 97

The growth of rat aorta vascular smooth muscle cells (VSMCs) was measured in the presence and absence of taurine. Concentrations of taurine as low as 0.3 mM in the culture medium inhibited the proliferation of the cells, as monitored by measuring cell count, and also inhibited the rate of DNA synthesis, as examined by measuring [3H]thymidine incorporation into DNA. However, even at the highest concentration of taurine (30 mM), the doubling time of the VSMCs was only increased by 38%. Protein content of the VSMCs was decreased by 30 mM taurine. [3H]Leucine incorporation into newly synthesized protein was not affected by the highest concentration of taurine tested (30 mM), indicating that taurine did not inhibit protein synthesis but rather decreased total protein content by inhibiting cellular proliferation. The effects of other amino acids such as alanine, glycine, and serine and of various taurine analogues such as beta-alanine, guanidinoethanesulfonic acid (GES), and isethionic acid also were tested at a concentration of 20 mM for their effects on the growth of the VSMCs. Alanine, glycine, and serine had only a minimal effect or no effect on cell count, quantity of protein, and incorporation of [3H]thymidine into DNA. GES, beta-alanine, and isethionic acid had a significant effect on cell count, protein content, and incorporation of [3H]thymidine into DNA. Beta-alanine was the only analogue tested that significantly depressed [3H]leucine incorporation into newly synthesized protein. It is concluded that taurine, GES, and isethionic acid inhibited proliferation of VSMCs but did not alter normal protein synthesis or survivability of VSMCs. In contrast, other amino acids, alanine, glycine and serine, had minimal effects on VSMC proliferation and protein synthesis, whereas beta-alanine appeared to be toxic, inhibiting both VSMC synthesis and de novo protein synthesis.
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PMID:Inhibition of rat vascular smooth muscle cell proliferation by taurine and taurine analogues. 1023 Jul 77

In search for more potent, particularly less ulcerogenic gastritis that hopefully replace the universal NSAID "Diclofenac", (2-[(2,6-dichlorophenyl)amino]-phenylacetic acid, C.A.S. 15307-86-5), twelve new non-proteinogenic amino acid conjugates of the drug, namely that of sarcosine, beta-alanine, D-leucine and D-phenylalanine, were synthesized and biologically screened for their anti-inflammatory, analgesic and ulcerogenic activity in rats. "Diclofenac" amino acid esters (IIa-d), were synthesized via the corresponding HOSu or HOBt active esters. Alkaline hydrolysis (NaOH) followed by acidification (KHSO4) or thioamide formation (Lawsson's Reagent, C.A.S. 19172-47-5), afforded the corresponding free acids IIIa-d or the thioamides IVa-d respectively. Interestingly, in contrary to the parent "Diclofenac", the synthesized candidates (except IIId), were entirely nonulcerogenic in rats. Further, they considerably retained a generalized anti-phlogistic activity. The major "Diclofenac" irritating gastric side effect was thus eliminated. Particularly, the sarcosine conjugate IIa and its thiomimic IVa exhibit promising therapeutic perspectives.
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PMID:Synthesis and anti-phlogistic potency of some new non-proteinogenic amino acid conjugates of "Diclofenac". 1039 25

In this study, a large number of polymeric chiral surfactants were examined and their performances in terms of enantiomeric resolution compared for a variety of chiral analytes. The surfactants investigated in this study include all possible dipeptide combinations of the L-form of alanine, valine, leucine, and the achiral amino acid glycine (except glycine-glycine). Also included in this study were the single amino acid surfactants of alanine, valine, and leucine as well as the single chiral center dipeptide surfactant poly(sodium undecyl-L-leucine-beta-alanine) (poly L-SULbetaA). Several different aspects of polymeric dipeptide surfactants, as they pertain to chiral separations, are examined. Some of the factors investigated in this report include the effect of position and number of chiral centers, amino acid order, and steric effects.
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PMID:Examination of structural changes of polymeric amino acid-based surfactants on enantioselectivity: effect of amino acid order, steric factors, and number and position of chiral centers. 1078 36

Although reports of decreased plasma taurine in trauma, sepsis and critical illness are available, very little is known about the relationships among changes in plasma taurine, other amino acid levels and metabolic variables. We analyzed a large series of plasma amino acid profiles obtained in trauma patients with sepsis who were undergoing total parenteral nutrition. The correlations between plasma taurine, other amino acid levels, parenteral substrate doses and metabolic and cardiorespiratory variables were assessed by regression analysis. Post-traumatic hypotaurinemia was followed by partial recovery toward less abnormal values when sepsis developed. Levels of taurine were directly and significantly related to levels of glutamate, aspartate, beta-alanine and phosphoethanolamine (and unrelated to other amino acids). Levels of these amino acids increased simultaneously with increasing doses of leucine, isoleucine and valine in total parenteral nutrition. Decreasing taurine was associated with increasing lactate, arteriovenous O(2) concentration difference and respiratory index, and with decreasing cholesterol and cardiac index. These results characterize the relationships between plasma taurine and other amino acid levels in sepsis, provide evidence of amino acid interactions that may support taurine availability and show more severe decreases in plasma taurine with the worsening of metabolic and cardiorespiratory patterns.
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PMID:The relationship between plasma taurine and other amino acid levels in human sepsis. 1095 16


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