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PubMed1991

The conformational stability and flexibility of insulin with an additional intramolecular cross-link.

The conformational stability and flexibility of insulin containing a cross-link between the alpha-amino group of the A-chain to the epsilon-amino group of Lys29 of the B-chain was examined. The cross-link varied in length from 2 to 12 carbon atoms. The conformational stability was determined by guanidine hydrochloride-induced equilibrium denaturation and flexibility was assessed by H2O/D2O amide exchange. The cross-link has substantial effects on both conformational stability and flexibility which depend on its length. In general, the addition of a cross-link enhances conformational stability and decreases flexibility. The optimal length for enhanced stability and decreased flexibility was the 6-carbon link. For the 6-carbon link the Gibbs free energy of unfolding was 8.0 kcal/mol compared to 4.5 kcal/mol for insulin, and the amide exchange rate decreased by at least 3-fold. A very short cross-link (i.e. the 2-carbon link) caused conformational strain that was detectable by a lack of stabilization in the Gibbs free energy of unfolding and enhancement in the amide exchange rate compared to insulin. The effect of the cross-link length on insulin hydrodynamic properties is discussed relative to previously obtained receptor binding results.

Animals↗
PubMed1990

Optimization of topical therapy: partitioning of drugs into stratum corneum.

To optimize a topical formulation for therapeutic effect generally implies that the flux of drug into the skin be maximized. This requirement means that the product of drug concentration in the vehicle (Cv) and drug partition coefficient (PC) between stratum corneum (SC) and vehicle be as large as possible. While Cv is a formulation variable which can be easily manipulated up to the drug's saturation solubility, PC is a parameter that is difficult to predict a priori. However, there is no question that an ability to evaluate PC would greatly facilitate the efficient screening of drugs and formulations. We have measured the SC/water and SC/isopropylmyristate (a model lipophilic vehicle) PCs of seven drugs; acitretin, progesterone, testosterone, diazepam, estradiol, hydrocortisone, and caffeine, SC/water PCs were determined as a function of the following variables: (i) initial drug concentration in the vehicle, (ii) length of equilibrium, (iii) SC source and preparation technique, and (iv) SC delipidization. The data obtained were reproducible and physicochemically consistent, and they show that useful partitioning information from both aqueous and nonaqueous vehicles can be obtained with the biological tissue of greatest relevance. The SC/water PCs of the steroids were in reasonable agreement with previous measurements. A facile approach to an integral determinant of formulation optimization is suggested, therefore, by these observations.

Administration, Cutaneous↗
PubMedDate not supplied

Contrast media in abdominal computed tomography: optimization of delivery methods.

OBJECTIVE: To provide a systematic overview of the effects of various parameters on contrast enhancement within the same population, an animal experiment as well as a computer-aided simulation study was performed. MATERIALS AND METHODS: In an animal experiment, single-level dynamic CT through the liver was performed at 5-second intervals just after the injection of contrast medium for 3 minutes. Combinations of three different amounts (1, 2, 3 mL/kg), concentrations (150, 200, 300 mgI/mL), and injection rates (0.5, 1, 2 mL/sec) were used. The CT number of the aorta (A), portal vein (P) and liver (L) was measured in each image, and time-attenuation curves for A, P and L were thus obtained. The degree of maximum enhancement (Imax) and time to reach peak enhancement (Tmax) of A, P and L were determined, and times to equilibrium (Teq) were analyzed. In the computed-aided simulation model, a program based on the amount, flow, and diffusion coefficient of body fluid in various compartments of the human body was designed. The input variables were the concentrations, volumes and injection rates of the contrast media used. The program generated the time-attenuation curves of A, P and L, as well as liver-to-hepatocellular carcinoma (HCC) contrast curves. On each curve, we calculated and plotted the optimal temporal window (time period above the lower threshold, which in this experiment was 10 Hounsfield units), the total area under the curve above the lower threshold, and the area within the optimal range. RESULTS: A. Animal Experiment: At a given concentration and injection rate, an increased volume of contrast medium led to increases in Imax A, P and L. In addition, Tmax A, P, L and Teq were prolonged in parallel with increases in injection time The time-attenuation curve shifted upward and to the right. For a given volume and injection rate, an increased concentration of contrast medium increased the degree of aortic, portal and hepatic enhancement, though Tmax A, P and L remained the same. The time-attenuation curve shifted upward. For a given volume and concentration of contrast medium, changes in the injection rate had a prominent effect on aortic enhancement, and that of the portal vein and hepatic parenchyma also showed some increase, though the effect was less prominent. A increased in the rate of contrast injection led to shifting of the time enhancement curve to the left and upward. B. Computer Simulation: At a faster injection rate, there was minimal change in the degree of hepatic attenuation, though the duration of the optimal temporal window decreased. The area between 10 and 30 HU was greatest when contrast media was delivered at a rate of 2-3 mL/sec. Although the total area under the curve increased in proportion to the injection rate, most of this increase was above the upper threshold and thus the temporal window was narrow and the optimal area decreased. CONCLUSION: Increases in volume, concentration and injection rate all resulted in improved arterial enhancement. If cost was disregarded, increasing the injection volume was the most reliable way of obtaining good quality enhancement. The optimal way of delivering a given amount of contrast medium can be calculated using a computer-based mathematical model.

Animals↗
PubMed1997

Characterization and optimization of phospholipase A2 catalyzed synthesis of phosphatidylcholine.

The phospholipase A2 (PLA2) catalyzed synthesis and hydrolysis of phosphatidylcholine (PC) was studied in a water activity controlled organic medium. The aim of the study was to find the conditions most favorable for the synthetic reaction. To do this, the impact of various parameters such as water activity, substrate concentration and temperature on enzyme activity and equilibrium yield was determined. The PC to lysophosphatidylcholine (LPC) ratio at equilibrium increases with decreasing water activity and increasing fatty acid concentration, as can be expected from the law of mass action of an esterification reaction. The enzyme activity on the other hand decreases under conditions that favor the esterification. The best yield in the synthetic reaction is 60% at a water activity of 0.11 and an oleic acid concentration of 1.8 M. That is to our knowledge the highest yield ever reported in this reaction. Both the hydrolysis and synthesis reaction follow Michaelis-Menten kinetics, the apparent Km values are the same for PC and LPC, namely 4.9 mM. Vmax is 82.5 and 10.4 nmol h(-1) mg(-1) for the hydrolysis and synthesis reaction, respectively. Studies on PLA2 at water activity controlled conditions resulted in a more complete understanding of the enzymatic reaction and allowed to find the conditions most favorable for the synthetic reaction.

Animals↗
PubMed2004

Complex folding pathways in a simple beta-hairpin.

The determination of the folding mechanisms of proteins is critical to understand the topological change that can propagate Alzheimer and Creutzfeld-Jakobs diseases, among others. The computational community has paid considerable attention to this problem; however, the associated time scale, typically on the order of milliseconds or more, represents a formidable challenge. Ab initio protein folding from long molecular dynamics simulations or ensemble dynamics is not feasible with ordinary computing facilities and new techniques must be introduced. Here we present a detailed study of the folding of a 16-residue beta-hairpin, described by a generic energy model and using the activation-relaxation technique. From a total of 90 trajectories at 300 K, three folding pathways emerge. All involve a simultaneous optimization of the complete hydrophobic and hydrogen bonding interactions. The first two pathways follow closely those observed by previous theoretical studies (folding starting at the turn or by interactions between the termini). The third pathway, never observed by previous all-atom folding, unfolding, and equilibrium simulations, can be described as a reptation move of one strand of the beta-sheet with respect to the other. This reptation move indicates that non-native interactions can play a dominant role in the folding of secondary structures. Furthermore, such a mechanism mediated by non-native hydrogen bonds is not available for study by unfolding and Gō model simulations. The exact folding path followed by a given beta-hairpin is likely to be influenced by its sequence and the solvent conditions. Taken together, these results point to a more complex folding picture than expected for a simple beta-hairpin.

Amino Acid Sequence↗
PubMed1999

Tetrameric N(5)-(L-1-carboxyethyl)-L-ornithine synthase: guanidine. HCl-induced unfolding and a low temperature requirement for refolding.

Guanidine x HCl (GdnHCl)-induced unfolding of tetrameric N(5)-(L-1-carboxyethyl)-L-ornithine synthase (CEOS; 141,300 M(r)) from Lactococcus lactis at pH 7.2 and 25 degrees C occurred in several phases. The enzyme was inactivated at approximately 1 M GdnHCl. A time-, temperature-, and concentration-dependent formation of soluble protein aggregates occurred at 0.5-1.5 M GdnHCl due to an increased exposure of apolar surfaces. A transition from tetramer to unfolded monomer was observed between 2 and 3.5 M GdnHCl (without observable dimer or trimer intermediates), as evidenced by tyrosyl and tryptophanyl fluorescence changes, sulfhydryl group exposure, loss of secondary structure, size-exclusion chromatography, and sedimentation equilibrium data. GdnHCl-induced dissociation and unfolding of tetrameric CEOS was concerted, and yields of reactivated CEOS by dilution from 5 M GdnHCl were improved when unfolding took place on ice rather than at 25 degrees C. Refolding and reconstitution of the enzyme were optimal at </=15 degrees C and yields of active tetramer increased as the concentration of unfolded subunits decreased. Refolding of unfolded subunits and active tetramer assembly upon 100-fold dilution from 5 M GdnHCl at 0 degrees C also was increased two- or fourfold (to 44 or 28% reactivation for 0.08 or 0.28 microM subunit, respectively) when incubated at 15 degrees C, pH 7.2, for 4 h with the Escherichia coli molecular chaperonin GroEL, ATP, MgCl(2), and KCl.

Amino Acid Oxidoreductases↗
PubMed1995

Purification and properties of insulin receptor ectodomain from large-scale mammalian cell culture.

Ectodomain of the exon 11+ form of the human insulin receptor (hIR) was expressed in the mammalian cell secretion vector pEE6.HCMV-GS, containing the glutamine synthetase gene. Following transfection of the hIR ectodomain gene into Chinese hamster ovary (CHO-K1) cells, clones were isolated by selecting for glutamine synthetase expression with methionine sulphoximine. The expression levels of ectodomain were subsequently increased by gene amplification. Production was scaled up using a 40-liter airlift fermenter in which the transfected CHO-K1 cells were cultured on microcarrier beads, initially in medium containing 10% fetal calf serum (FCS). By continuous perfusion of serum-free medium into the bioreactor, cell viability was maintained during reduction of FCS, which enabled soluble hIR ectodomain to be harvested for at least 22 days. Harvests were concentrated 20-fold by anion-exchange chromatography. Optimal recovery of ectodomain from early harvests containing large quantities of serum proteins was achieved by insulin-affinity chromatography, whereas in later harvests purification was achieved by multistep chromatography. Analysis of the purified hIR ectodomain showed that it had a molecular weight by sedimentation equilibrium analysis of 269,500. Amino-terminal amino acid sequence analysis showed that the ectodomain was correctly processed to alpha and beta chains and that glycosylation characteristics were similar to those of native hIR. The integrity of the ectodomain was demonstrated by the recognition of conformation-dependent anti-hIR antibodies and by its binding of insulin (Kd approximately 2 x 10(-9) M). These results demonstrate the successful production and purification of hIR ectodomain by processes amenable to scale-up and in a form appropriate for structure/function studies of the ligand-binding domain of the receptor.

Animals↗
PubMed1983

Analysis of numerical methods for computer simulation of kinetic processes: development of KINSIM--a flexible, portable system.

A flexible and convenient computational method for the simulation of kinetic progress curves has been developed. A mechanism is represented in conventional chemical format with either kinetic or rapid equilibrium steps separating chemical species. A table describing the differential equations of the mechanism is generated and a direct numerical integration is performed. The same program can be used to simulate any number of mechanisms. The user may interactively set kinetic parameters to seek the optimal fit for a set of experiments, as determined by graphical superimposition of simulated curves with experimental data. Standard error analysis and automatic optimization may also be included. The program is computationally efficient and its interactive nature makes it a good teaching tool. The source code is written in FORTRAN IV and adheres closely with the ANSI 1966 standard, so as to make it maximally portable and machine independent.

Chemistry Techniques, Analytical↗
PubMed1996

Validation of a three-dimensional model of the knee.

Three-dimensional mathematical models of the tibio-femoral joint require input of the geometry of articulating surfaces and ligament insertions, and the mechanical properties of cartilage and ligaments. This paper describes a validation of a knee model through a direct specimen-related comparison between the knee model and the kinematics of four knee joint specimens from which the geometry data were used as input of the model. The knee model is quasi-static and is based on equilibrium of forces and moments. The stiffness properties of the ligaments and articular cartilage were estimated on the basis of data reported in the literature. The so-called reference strains in the ligament bundles for the joint in extension, were determined by using an optimization procedure, minimizing the difference between the kinematics of the model and the kinematics of experimentally obtained flexion motions with an internally or an externally rotated tibia (+/- 3 Nm load). A reasonable to good agreement between the model and the experimental kinematics could be obtained for internal-external rotation laxity and the coupled translations and varus-valgus rotation. The disparity between model and experiment varied from knee to knee, average deviations ranging from close to zero to 8 degrees internal rotation deviation and from 5 mm posterior to 3 mm anterior position deviation. The average anterior-posterior laxities at both 20 degrees and 90 degrees flexion were within the variations reported in the literature, although for each individual joint with some underestimation or overestimation. It was concluded that the optimization procedure compensated for the lack of menisci and capsular structures by higher prestrains, thereby overestimating the ligament forces. Despite the gross simplifications relative to the complex anatomy of the knee, the present knee model can realistically simulate the passive motion characteristics of the human knee joint.

Elasticity↗
PubMedDate not supplied

A computational study of intramolecular proton transfer in gaseous protonated glycine.

The minimum energy paths for intramolecular proton transfer between the amino nitrogen and carbonyl oxygen atoms in gaseous protonated glycine were estimated at the Hartree-Fock (HF) and second-order Møller-Plesset Perturbation (MP2) levels of theory. Potential energy profiles and their associated reactant, transition state, and product species calculated at the MP2/6-31G* level were shown to differ significantly from those obtained at the HF/6-31G* level. Effects of electron correlation and basis functions on the calculated geometries and energies of relevant species were examined at the HF, MP2, MP4, CCSD, and B3LYP levels using the 6-31G*, 6-31G**, 6-31+G**, 6-311+G**, 6-31+G(2d,2p), 6-311+G(3df,2p), cc-pVDZ, aug-cc-pVDZ, and cc-pVTZ basis sets. The HF and MP2 optimized levels with the 6-31G*, 6-31G**, 6-31+G**, and 6-311+G** bases were used to calculate the thermodynamic and kinetic properties of the proton transfer reaction at 298.15 K and 1 atm, which include enthalpy, entropy, Gibbs free energy, equilibrium constant, potential energy barriers, tunneling transmission coefficients, and rate constants. Results indicate that the proton in a carbonyl O-protonated glycine undergoes a rapid migration to the amino nitrogen atom, while the reverse process is extremely unfavorable. The objective of this work is to develop practical theoretical procedures for studying proton transfer reactions in amino acids and peptides and to assemble physical data from these model calculations for future references.

Electrochemistry↗
PubMed2006

Defect disorder of titanium dioxide.

The present work derived defect disorder diagram representing the effect of oxygen activity on the concentration of both ionic and electronic defects for undoped TiO2. This diagram was determined using the equilibrium constants derived in the present work, including (i) the intrinsic electronic equilibrium constant, (ii) the equilibrium constant for the formation of oxygen vacancies, and (iii) equilibrium constant for the formation of titanium vacancies. These equilibrium constants are consistent with three properties determined independently, including: electrical conductivity, thermoelectric power and change of mass determined by thermogravimetry. The derived defect disorder diagram may be used for tailoring semiconducting properties of TiO2 that are desired for specific applications through the selection of optimized processing conditions.

Journal Article↗
PubMed2003

Interaction of bacteriochlorophyll with the LH1 and PufX polypeptides of photosynthetic bacteria: use of chemically synthesized analogs and covalently attached fluorescent probes.

The protein components of the reaction center (RC) and core light-harvesting (LH 1) complexes of photosynthetic bacteria have evolved to specifically, but non-covalently, bind bacteriochlorophyll (Bchl). The contribution to binding of specific structural elements in the protein and Bchl may be determined for the LH 1 complex because its subunit can be studied by reconstitution under equilibrium conditions. Important to the determination and utilization of such information is the characterization of the interacting molecular species. To aid in this characterization, a fluorescent probe molecule has been covalently attached to each of the LH 1 polypeptides. The fluorescent probes were selected for optimal absorption and emission properties in order to facilitate their unique excitation and to enable the detection of energy transfer to Bchl. Oregon Green 488 carboxylic acid and 7-diethylaminocoumarin-3-carboxylic acid seemed to fulfill these requirements. Each of these probes were utilized to derivatize the LH1 beta-polypeptide of Rhodobacter sphaeroides. It was demonstrated that the beta-polypeptides did not interact with each other in the absence of Bchl. When Bchl was present, the probe-labeled beta-polypeptides interacted with Bchl to form subunit-type complexes much as those formed with the native polypeptides. Energy transfer from the probe to Bchl occurred with a high efficiency. The alpha-polypeptide from LH 1 of Rb. sphaeroides and that from Rhodospirillum rubrum were also derivatized in the same manner. Since these polypeptides do not oligomerize in the absence of a beta-polypeptide, reversible binding of a single Bchl to a single polypeptide could be measured. Dissociation constants for complex formation were estimated. The relevance of these data to earlier studies of equilibria involving subunit complexes is discussed. Also involved in the photoreceptor complex of Rb. sphaeroides and Rhodobacter capsulatus is another protein referred to as PufX. Two large segments of this protein were chemically synthesized, one reproducing the amino acid sequence of the core segment predicted for Rb. sphaeroides PufX and the other reproducing the amino acid sequence predicted for the core segment of Rb. capsulatus PufX. Each polypeptide was covalently labeled with a fluorescent probe and tested for energy transfer to Bchl. Each was found to bind Bchl with an affinity similar to the affinity of the LH 1 polypeptides for Bchl. It is suggested that PufX binds Bchl and interacts with a Bchlcalpha-polypeptide component of LH 1 to truncate, or interupt, the LH 1 ring adjacent to the location of the Q(B) binding site of the RC.

Journal Article↗
PubMed2005

Field enhancements of packed-bed performance for low-concentration acidic and basic-waste gases from semiconductor manufacturing process.

Low-concentration acidic and basic-waste gas pollutants contribute significantly in the total emission of a facility. Previous results show that the control of high volumetric flow rate (approximately 500 m3/min), low-concentration acidic (< 1 ppm by vol) and basic (< 3 ppm by vol) gases from semiconductor process vent, by conventional wet scrubbing technique is a challenging task. This work was targeted to enhance the performance of packed beds for high-volumetric flow rate, low-concentration acidic (HF, HCl), and basic (NH3)-waste gases from the semiconductor manufacturing process. The methodology used to meet the goal was the application of fine-water mist over the inlet stream before entering to the packed bed and use of the surfactant with mist/packed-bed liquid in low concentration. An experimental study was carried out in two acid-packed beds to optimize the operating conditions, such as pH of the liquid, circulating liquid flow rate, blow-down cycle, and so forth. The relationship among liquid pH, liquid ionic concentration, and the removal efficiency of the packed bed for the pollutants has been discussed considering chemical equilibrium, two-film theory, and Henry's law. For the potential utilization of scrubbing water, the dependency of the efficiency on blow-down cycle was studied, and a mechanism is suggested. The proposed water-mist surfactant system was installed in two acid-packed beds, and performance of the packed beds was compared. The background efficiencies of the acid-packed beds for HF, HCl, and NH3 were found max to be (n = 11) 53, 40, and 27%, whereas after installation of the system, they increased significantly and became 76 +/- 13% (n = 10), 76 +/- 8% (n = 7), and 78 +/- 7% (n = 7), respectively, for inlet concentrations of HF and HCl < 1 ppm and NH3 < 14 ppm. The mechanism by which the surfactants operate to enhance the removal in scrubbing process is suggested considering the hydrodynamic effect and the interfacial effect with the charge-generating characteristic of surfactants on water surface, when dissolved into water. The results show that a proposed rectification system can effectively reduce the emission rates below the regulatory level (0.6 kg/hr) at the present conditions of the facility.

Air Movements↗
PubMed1985

Enzymic Properties of Ribulose-1,5-bisphosphate Carboxylase/Oxygenase Purified from Rice Leaves.

The enzymic properties of ribulose 1,5-bisphosphate (RuBP) carboxylase/oxygenase purified from rice (Oryza sativa L.) leaves were studied. Rice RuBPcarboxylase, activated by preincubation with CO(2) and Mg(2+) like other higher plant carboxylases, had an activation equilibrium constant (K(c)K(Mg)) of 1.90 x 10(5) to 2.41 x 10(5) micromolar(2) (pH 8.2 and 25 degrees C). Kinetic parameters of carboxylation and oxygenation catalyzed by the completely activated enzyme were examined at 25 degrees C and the respective optimal pHs. The K(m)(CO(2)), K(m)(RuBP), and V(max) values for carboxylation were 8 micromolar, 31 micromolar, and 1.79 units milligram(-1), respectively. The K(m)(O(2)), K(m)(RuBP), and V(max) values for oxygenation were 370 micromolar, 29 micromolar, and 0.60 units milligram(-1), respectively.Comparison of rice leaf RuBP carboxylase with other C(3) plant carboxylases showed that it had a relatively high affinity for CO(2) but the lowest catalytic turnover number (V(max)) among the species examined.

Journal Article↗
PubMed1982

Binding of human factor VII and VIIa to monocytes.

Human coagulation Factors VII and VIIa bind with equal affinity to monocytes stimulated with endotoxin. Equilibrium binding studies performed at 0 degrees C using 125I-labeled Factor VII and VIIa showed the dissociation constant (Kd) to be congruent to 82 pM with congruent to 3,600 binding sites/monocyte. Ca++ was required for Factor VII and VIIa interaction with monocytes (optimal CaC12 concentration greater than or equal to 2.5 mM) and binding was reversed by the addition of EDTA. The rate of conversion of Factor X to Xa in mixtures containing Factor VIIa and monocytes was directly related to the quantity of Factor VIIa bound to the monocyte surface. Thus the monocyte binding sites appear to represent tissue factor. Competition experiments showed that Factor VII and VIIa bind to the same monocyte sites and further, that unlabeled Factor VII and VIIa have the same affinity for the binding sites as the 125I-labeled proteins.

Binding, Competitive↗
PubMed1984

Triphenylethylene antiestrogen-binding sites in cockerel liver nuclei: evidence for an endogenous ligand.

Salt extracts of purified nuclei from cockerel liver contain a limited number of sites that bind triphenylethylene nonsteroidal antiestrogens with high affinity and specificity. The assay of the [3H]tamoxifen (3H-labeled 1-[4-(2-dimethylaminoethyoxy)phenyl] 1,2-diphenylbut-1-(Z)ene)-binding sites is optimally achieved by preincubation of the salt extracts with charcoal-dextran suspension; a 4- to 8-fold increase in activity over that obtained with nontreated extracts is found. This suggests that the binding sites are occupied in vivo by an unknown endogenous ligand. The equilibrium dissociation constant for [3H]tamoxifen binding is 4.76 +/- 1.8 nM, and the binding site concentration is 1.7 +/- 0.7 fmol/microgram DNA. The concentration of high affinity estrogen-binding sites in the same extracts is almost 30-fold less (0.06 +/- 0.01 fmol/micrograms DNA). The relative binding affinities of various antiestrogens for the nuclear antiestrogen-binding sites (with tamoxifen arbitrarily set at 100%) are as follows: nafoxidine (1-[2-(p-[3,4-dihydro-6-methoxy-2-phenyl-1-naphthyl]phenoxy)ethyl] pyrrolidine hydrochloride); 126%) greater than tamoxifen (100%) greater than N-des-methyltamoxifen (16%) greater than CI-628 (alpha-[p-[2-(1-pyrrolidine)ethyoxy]phenyl] 4-methoxy-alpha'-nitrostilbene; 14%) greater than 4-hydroxytamoxifen (7%). Estrogens (17 beta-estradiol, estriol, estrone, and diethylstilbestrol) and several other steroids (cholesterol, dihydrotestosterone, pregnenolone, progesterone, and hydrocortisone) show little or no affinity for binding to the nuclear sites (relative binding affinity, less than 0.5%). However, ether extracts of cockerel serum or liver nuclei contain a substance(s) that competitively inhibits [3H]tamoxifen binding to the nuclear antiestrogen-binding sites. The ether-soluble material does not compete for [3H]estradiol binding to the salt-soluble nuclear estrogen receptor. These studies suggest that cockerel serum and liver nuclei contain a natural compound which competes with the triphenylethylenes at the antiestrogen-binding site and may occupy the nuclear binding sites in vivo.

Animals↗
PubMed2002

Adequacy of hemodialysis.

The concept adequate includes blood purification, maintenance of electrolyte fluid, and acid-base equilibrium. Dialysis can completely reverse the retention of some small molecules, electrolytes (K, Na, Mg), water and acid-base, and has no effect on anemia, hypertension, arteriosclerosis, cardiomyopathies, malnutrition, bleeding, or partial effect on Ca-P balances. Other therapeutic interventions are necessary to optimally treat the uremic syndromes. Urea kinetic modelling is probably the most objective way of measuring the efficiency of dialysis but we must remember that there are numerous alterations in ESRD which cannot be measured by urea kinetic modelling.

Body Fluid Compartments↗
PubMed1990

Continuous synthesis of a tripeptide by successive condensation and transesterification catalyzed by two immobilized proteinases in organic solvent.

The tripeptide Z-GlyPheLeuNH2 was continuously synthesized in a high yield from three amino acid derivatives, Z-Gly, PheOMe, and LeuNH2, by immobilized thermolysin (IMT) and immobilized alpha-chymotrypsin (IMC) in an organic solvent, ethyl acetate. The optimal conditions for the synthesis of Z-GlyPheOMe were established theoretically. The yield of Z-GlyPheOMe with IMT in ethyl acetate saturated with buffer was more than 88% after continuous synthesis for 116 hr. The optimal conditions for the synthesis of Z-GlyPheLeuNH2 from Z-GlyPheOMe and LeuNH2 by IMC through transesterification was established in batch reaction experiments. When the concentration of water in the reaction solution was 17-20 microliters/ml, the activity of IMC was highest. The equilibrium between the water concentration in the reaction solution and that in the resin used for enzyme immobilization depended on the resin and was not affected by the presence of the enzyme immobilized. Z-GlyPheLeuNH2 was synthesized from Z-GlyPheOMe and LeuNH2 with a yield of 100%, by continuous reaction for 160 hr. The reactor for synthesis of this tripeptide was efficient and stable because of the use of transesterification and the choice of an appropriate organic solvent. The series plug-flow reactor was successfully operated for 220 hr with a yield of more than 80%. The residual activity of IMT was 94% and that of IMC was 100%.

Acetates↗