Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027960 (mole)
 21,279 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Sheep ovarian 17 beta HSDH has been purified about 1000 fold to a specific activity of 0.5 IU/mg protein, using DEAE cellulose chromatography, affinity chromatography on estrone-amino caproate-Sepharose and a second DEAE cellulose chromatography. The molecular weight is 70,000 ; the pH optimum for activity is 9.2 and the energy of activation is 16.5 Kcal/mole. The kinetics of the oxidation of estradiol and many analogues have been studied at various concentrations and in the presence of different amounts of coenzyme. The data are in agreement with a compulsory order mechanism with the binding of NAD+ as the first substrate. Sheep ovarian 17 beta HSDH accepts subtituents in position C3, C11, C13 ; the substrate binding site is open in this region. On the contrary, the binding requirements are strict for the region of C10 since the presence of a C19 methyl group impairs binding and (or) oxidation of the steroid. Sheep ovarian and human placental 17 beta HSDH have close analogies : molecular weight, pH optimum, substrate binding site requirements. Their reaction mechanisms are different : random for the placental 17 beta HSDH, compulsory order for the ovarian 17 beta HSDH : this can be explained by the effect of the coenzyme upon the binding of the substrate : without effect on placental enzyme, the coenzyme fixation enhances the affinity of the ovarian 17 beta HSDH for any substrate.
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PMID:17 beta-Hydroxysteroid dehydrogenase of the sheep ovary : purification, properties and substrate binding site. 0 49

Temperature-jump relaxation experiments on Na+ transport by (221)C10-cryptand were carried out in order to study the influence of cholesterol and its temperature-dependence on ion transport through thin lipid membranes. The experiments were performed on large, negatively charged unilamellar vesicles (LUV) prepared from mixtures of dioleoylphosphatidylcholine, phosphatidic acid and cholesterol (mole fractions 0-0.43), at various temperatures and carrier concentrations. The initial rates of Na+ transport and the apparent rate constants of its translocation by (221)C10 increased with the carrier concentration and the temperature. The incorporation of cholesterol into the membranes significantly reduced the carrier concentration- and temperature-dependence of these two parameters. The apparent energy required to activate the transport decreased significantly with increasing carrier concentrations at any given cholesterol molar fraction, and increased significantly with the cholesterol molar fraction at any given carrier concentration. Our interpretation of the action of cholesterol on this transport system is based on the assumption that the binding cavity of cryptands is likely to be located towards the aqueous side of the dipole layer. The results are discussed in terms of the structural, physico-chemical and electrical characteristics of carriers and complexes, and of the interactions occurring between an ionizable mobile carrier and the membrane.
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PMID:Temperature-dependent effects of cholesterol on sodium transport through lipid membranes by an ionizable mobile carrier. 150 75

Nucleosomal-length DNA was constructed to contain one of two 10 bp oligopurine-oligopyrimidine sequences, either d(A10.T10) or d(G10.C10). The 146 base pair (bp) sequences were then each tandemly cloned. This allowed for the production of circularly-permuted sequence variants in which the oligopurine tract was located at eight different positions. The permuted sequences were then assayed for their ability to reconstitute into nucleosomes by competitive reconstitution. The results of the assay indicate that the free energy of nucleosome formation differs only by several tenths of a kilocalorie per mole for an oligopurine tract at any position along the DNA, including the central dyad region.
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PMID:Isolated oligopurine tracts do not significantly affect the binding of DNA to nucleosomes. 160 63

Rotational diffusion of androstane spin-label (ASL), a sterol analogue, in various phosphatidylcholine (PC)-cholesterol membranes was systematically studied by computer simulation of steady-state ESR spectra as a function of the chain length and unsaturation of the alkyl chains, cholesterol mole fraction, and temperature for a better understanding of phospholipid-cholesterol and cholesterol-cholesterol interactions. Special attention was paid to the differences in the cholesterol effects on ASL motion between saturated and unsaturated PC membranes. ASL motion in the membrane was treated as Brownian rotational diffusion of a rigid rod within the confines of a cone imposed by the membrane environment. The wobbling rotational diffusion constant of the long axis, its activation energy, and the cone angle of the confines were obtained for various PC-cholesterol membranes in the liquid-crystalline phase. Cholesterol decreases both the cone angle and the wobbling rotational diffusion constant for ASL in all PC membranes studied in this work. The cholesterol effects are the largest in DMPC membranes. An increase of cholesterol mole fraction from 0 to 30% decreases the rotational diffusion constant by a factor of 9-15 (depending on temperature) and the cone angle by a factor of about 2. In dioleoyl-PC membranes, addition of 30 mol % cholesterol reduces both the rotational diffusion constant and the cone angle of ASL by factors of approximately 2.5 and approximately 1.3, respectively, while it was previously found to cause only modest effects on the motional freedom of phospholipid analogue spin probes [Kusumi, A., Subczynski, W. K., Pasenkiewicz-Gierula, M., Hyde, J. S., & Merkle, H. (1986) Biochim. Biophys. Acta 854, 307-317]. It is proposed that fluid-phase microimmiscibility takes place in dioleoyl-PC-cholesterol membranes at physiological temperatures, which induces cholesterol-rich domains in the membrane, partially due to the steric nonconformability between the rigid fused-ring structure of cholesterol and the 30 degrees bend at the C9-C10 cis double bond of the alkyl chains of dioleoyl-PC. The mechanism by which cholesterol influences the lipid dynamics in the membrane is different between saturated and unsaturated PC membranes.
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PMID:Rotational diffusion of a steroid molecule in phosphatidylcholine-cholesterol membranes: fluid-phase microimmiscibility in unsaturated phosphatidylcholine-cholesterol membranes. 216 71

The inhibition of dansylsarcosine (DS) binding at the benzodiazepine binding site of human serum albumin has been studied in the presence of saturated and unsaturated free fatty acids (FFA) of various chain lengths (C6-C20, C18:1, C18:2). In order to determine the mechanism of displacement, velocity constants for association (k2) and dissociation (k-2) and binding constants (KA and KA') have been measured using the stopped-flow method. The inhibitory effect of FFA on DS binding kinetics at site II is dependent of their structure. With increasing amounts of FFA the association velocity constant of DS binding decreases from 520 s-1 (fatty acid free albumin) by a factor of 3-10 and affinity decreases according to FFA chain length. Inhibition is strongest in the presence of caprylic, capric and lauric acid (C8-C12) i.e. with more than one mole FFA per mole albumin, DS association could no longer be measured. Short chain caproic and the long chain FFA C14-C20 showed only a less inhibitory effect since in the presence of a twofold excess k2 ranged between 100 and 200 s-1. Dissociation velocity of DS from the benzodiazepine binding site could be measured in relationship to FFA chain length using ibuprofene, another drug binding at site II. Dissociation velocity constants k-2 remained constant up to 2 moles FFA per mole albumin (k-2 = 16-18 s-1). A rise in k-2 to 70 s(-1) was seen, however, when 2-4 moles capric, lauric, myristic and palmitic (C10-C16) acid were bound, whereas no change was observed when increasing concentrations of caproic, caprylic, stearic and arachic acid.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Kinetics of drug binding to human serum albumin: allosteric and competitive inhibition at the benzodiazepine binding site by free fatty acids of various chain lengths. 247 Oct 88

The kinetics of Na+ and K+ transport across the membrane of large unilamellar vesicles (LUV) were determined at two pH's when transport was induced by (221)C10-cryptand (diaza-1,10-decyl-5-pentaoxa-4,7,13,16,21-bicyclo [8.8.5.] tricosane) at various temperatures, and by nonactin at 25 degrees C and (222)C10-cryptand at 20 and 25 degrees C. The rate of Na+ and K+ transport by (221)C10 saturated with the cation and carrier concentrations. Transport was noncooperative and exhibited selectivity for Na+ with respect to K+. The apparent affinity of (221)C10 for Na+ was higher and less pH-dependent than that for K+, and seven times higher than the affinity for Na+ of nonactin. Its enthalpy was higher than that of (222)C10 for K+ ions (20.5 vs. 1.7 kcal . mole-1). The efficiency of (221)C10 transport of Na+ was pH- and carrier concentration-dependent, and was similar to that of nonactin; its activation energy was similar to that for (222)C10 transport of K+ (35.5 and 29.7 kcal . mole-1, respectively). The reaction orders in cation n(S) and in carrier m(M), respectively, increased and decreased as the temperature rose, and were both independent of carrier or cation concentrations; in most cases, they varied slightly with the pH. n(S) varied with the cation at pH 8.7 and with the carrier for Na+ transport only, while m(M) always depended on the type of cation and carrier. Results are discussed in terms of the structural, physico-chemical and electrical characteristics of carriers and complexes.
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PMID:Efficiency, Na+/K+ selectivity and temperature dependence of ion transport through lipid membranes by (221)C10-cryptand, an ionizable mobile carrier. 344 19

The hydrophobicity profiles across phosphatidylcholine (PC)-cholesterol bilayer membranes were estimated in both frozen liposome suspensions and fluid-phase membranes as a function of alkyl chain length, unsaturation, and cholesterol mole fraction. A series of stearic acid spin labels, with the probe attached to various positions along the alkyl chain, cholesterol-type spin labels (cholestane and androstane spin labels), and Tempo-PC were used to examine depth-dependent changes in local hydrophobicity, which is determined by the extent of water penetration into the membrane. Local hydrophobicity was monitored primarily by observing the z component of the hyperfine interaction tensor (Az) of the nitroxide spin probe in a frozen suspension of the membrane at -150 degrees C and was further confirmed in the fluid phase by observing the rate of collision of Fe(CN)6(3-) with the spin probe in the membrane using saturation recovery ESR. Saturated-PC membranes show low hydrophobicity (high polarity) across the membrane, comparable to 2-propanol and 1-octanol, even at the membrane center where hydrophobicity is highest. Longer alkyl chains only make the central hydrophobic regions wider without increasing the level of hydrophobicity. Introduction of a double bond at C9-C10 decreases the level of water penetration at all locations in the membrane, and this effect is considerably greater than the cis configuration than with the trans configuration. Incorporation of cholesterol (30 mol %) dramatically changes the profiles; it decreases hydrophobicity (increases water penetration) from the polar headgroup region to a depth of approximately C7 and C9 for saturated- and unsaturated-PC membranes, respectively, which is about where the bulky rigid steroid ring structure of cholesterol reaches in the membrane. Membrane hydrophobicity sharply increases at these positions from the level of methanol to the level of pure hexane, and hydrophobicity is constant in the inner region of the membrane. Thus, formation of effective hydrophobic barriers to permeation of small polar molecules requires alkyl chain unsaturation and/or cholesterol. The thickness of this rectangular hydrophobic barrier is less than 50% of the thickness of the hydrocarbon regions. Results obtained in dioleoyl-PC-cholesterol membranes in the fluid phase are similar to those obtained in frozen membranes. These results correlate well with permeability data for water and amino acids in the literature.
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PMID:Hydrophobic barriers of lipid bilayer membranes formed by reduction of water penetration by alkyl chain unsaturation and cholesterol. 801 34

Temperature-jump relaxation experiments on Na+ transport by (221)C10-cryptand (ionizable mobile carrier) and nonactin (neutral mobile carrier) were carried out in order to study the effects of cholesterol and the degree of acyl chain unsaturation, and their temperature-dependence on ion transport through thin lipid membranes. The experiments were performed on large, negatively charged unilamellar vesicles (LUV) prepared from mixtures of phosphatidylcholine (egg phosphatidylcholine, dioleoylphosphatidylcholine and dilinoleolylphosphatidylcholine), phosphatidic acid and cholesterol (mole fractions 0-0.43), at various temperatures and carrier concentrations. The apparent rate constants of Na+ translocation by (221)C10 and nonactin increased with the carrier concentration, the degree of acyl chain unsaturation and the temperature. The incorporation of cholesterol into the membranes significantly reduced the carrier concentration-, acyl chain unsaturation- and temperature-dependence of this parameter. The apparent energy required to activate the transport decreased significantly with increasing (221)C10 concentrations and remained constant with increasing those of nonactin at any given cholesterol molar fraction and degree of acyl chain unsaturation. It increased significantly with increasing the cholesterol molar fraction at any given carrier concentration to an extent depending on the degree of acyl chain unsaturation. Our interpretation of the action of cholesterol on these transport systems is based on the assumption that the adsorption plane of Na(+)-(221)C10 and Na(+)-nonactin complexes is likely to be located towards the aqueous and the hydrocarbon side of the dipole layer, respectively. The results are discussed in terms of the structural, physico-chemical and electrical characteristics of carriers and complexes, and of the interactions occurring between an ionizable or a neutral mobile carrier and the membrane.
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PMID:Sodium transport by an ionizable and a neutral mobile carrier: effects of membrane structure on the apparent activation energy. 844 24

Capric acid (C10:0) was incorporated into rice bran oil with an immobilized lipase from Rhizomucor miehei as the biocatalyst. Effects of incubation time, substrate mole ratio, enzyme load, and water addition on mole percent incorporation of C10:0 were studied. Transesterification was performed in an organic solvent, hexane, and under solvent-free condition. Pancreatic lipase-catalyzed sn-2 positional analysis and tocopherol analysis were performed before and after enzymatic modification. Products were analyzed by gas-liquid chromatography (GLC) for fatty acid composition. After 24 h of incubation in hexane, there was an average of 26.5 +/- 1.8 mol % incorporation of C10:0 into rice bran oil. The solvent-free reaction produced an average of 24.5 +/- 3.7 mol % capric acid. In general, as the enzyme load, substrate mole ratio, and incubation time increased, the mole percent of capric acid incorporation also increased. Time course reaction indicated C10:0 incorporation increased up to 27.0 mol % at 72 h, for the reaction in hexane, and up to 29.6 mol % at 12 h, for the solvent-free reaction. The highest C10:0 incorporations (53.1 and 43.2 mol %) for the mole ratio experiment occurred at a mole ratio of 1:8 for solvent and solvent-free reactions, respectively. The highest C10:0 incorporation (27.9 mol %) for the reaction in hexane occurred at 10% enzyme load, and the highest incorporation (34.4 mol %) for the solvent-free reaction occurred at 20% enzyme load. Incorporation of C10:0 into rice bran oil declined with the addition of increasing amounts of water after reaching 30.3 mol % at 2% water addition in hexane, and in the solvent-free reaction after reaching 35.9 mol %.
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PMID:Lipase-catalyzed modification of rice bran oil to incorporate capric acid. 1099 76

The detailed interfacial adsorption and micellization behavior of pure and mixed alkyltrimethylammonium bromides (ATABs: C10-, C12-, C14-, and C16TAB) were studied using tensiometric, conductometric, fluorimetric, viscometric, and calorimetric methods. The critical micellar concentration (CMC), thermodynamics of adsorption and micellization, counterion binding, aggregation number, and micellar polarity were determined. It was observed that the studied 1:1 molar mixtures of C10-C12TAB, C10-C14TAB, and C10-C16TAB, and the mixtures C12-C14TAB and C12-C16TAB at different mole ratios produced two CMCs that were supported by the conductometric, calorimetric and viscometric methods. Compared to the first micelle, the second micelle condensed more counterions and produced a higher aggregation number, but their interior polarity states were the same. The surface excess, area minimum of the ATABs at the CMC and Gibbs free energy of adsorption were evaluated and compared. The ideality/nonideality states of the mixed micelles formed in solution were tested in the light of Clint and Rubingh's formalisms; the mixed systems were found to undergo moderate to weak synergistic interaction. The contributions of the terminal methyl group, the intermediate methylene groups, and the hydrophilic tetramethylammonium group toward the standard Gibbs free energy, enthalpy, and entropy of the micellization processes were deciphered and discussed.
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PMID:Self-aggregation of alkyltrimethylammonium bromides (C10-, C12-, C14-, and C16TAB) and their binary mixtures in aqueous medium: a critical and comprehensive assessment of interfacial behavior and bulk properties with reference to two types of micelle formation. 1628 59


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