• Archives of Pharmacal Research
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• v.21 no.4
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• pp.465-469
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• 1998

The search for platinum (II)-based compounds with improved therapeutic properties was prompted to design and synthesize a new family of water-soluble, third generation cis-diaminedichloroplatinum (II) complexes linked to uracil and uridine. Six heretofore unreported uracil and uridine-platinum (II) complexes are; [N-(uracil-5-yl-methyl)ethane-1,2-di-amine]dichloroplatinum (II) (3a), [N-(uracil-6-yl-methyl)ethane-1,2-diaminel dichloroplatinum (II) (3b), t[N-($2^1$, $3^1$,$5^1$-tri-O-acetyl)uridine-5-yl-methyl] ethane-1,2-diamineldichloroplatinum (II) (6a), {[N-($2^1$,$3^1$, $5^1$-tri-O-acetyl) uridine-6-yl-methyl]ethane-1,2-diamine)dichloroplatinum (II) (6b),[N-(uridine- 5-yl-methyl)ethane-1,2-diamine]dichloroplatinum (II) (7a), [N-(uridine-6-yl- methyl)ethane-1,2-diamine]dichloroplatinum (II) (7b). These analogues were prepared from the key starting materials, 5-chloromethyluracil (1a) and 6-chloromethyluracil (1b) which were reacted with ethylenediamine to afford the respective 5-[(2-aminoethyl)aminol methyluracil (2a) and 6-[(2-aminoethyl)amino]methyluracil (2b). The cis-platin complexes 3a and 3b were obtained through the reaction of the respective 2a and 2b with potassium tetrachloroplatinate (II). The heterocyclic nucleic acid bases 1a and 1b were efficiently introduced on the .betha.-D-ribose ring via a Vorbruggen-type nucleoside coupling procedure with hexamethyldisilazane, trimethylchlorosilane and stannic chloride under anhydrous acetonitrile to yield the stereospecific .betha.-anomeric 5-chloromethyl- $2^1$,$3^1$,$5^1$-tri-O-acetyluridine (4a) and 6-chloromethyl-$2^1$,$3^1$,$5^1$-tri-O-acetyluridine (4b), respectively. The nucleosides 4a and 4b were coupled with ethylenediamine to provide the respective 5-[(amino-ethyl)aminolmethyl-$2^1$,$3^1$,$5^1$-tri-O-acetyluridine (5a) and 6-[(aminoethyl)amino] methyl-$2^1$,$3^1$,$5^1$-tri-O-acetyluridine (5b). The diamino-uridines 5a and 5b were reacted with potassium tetrachloroplatinate (II) to give the novel nucleoside complexes, 6a and 6b, respectively which were deacetylated into the free nucleosides, 7a and 7b by the treatment with CH$_{3}$ONa. The cytotoxic activities were evaluated against three cell lines (FM-3A, P-388 and J-82) and none of the synthesized compounds showed any significant activity.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.11 no.11
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• pp.4656-4663
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• 2010

In this study, the 3D computational fluid dynamics (CFD) was performed in relation to the internal fluid characteristics, flow distribution, air mean ages, and residence time for the development of the most optimal model in the complex post-disposal device. As it is expected that a channeling (drift) would be made by the semi-dry reactor due to the large difference in the flow distribution by the compartment in the bag filter, a structural improvement should be urgently made for more uniformed flow distribution in the bag filter. In addition, it showed the possibility that the velocity field and distribution characteristics of the residence time could be improved through a modification to inlet structure of the spray dryer reactor. The complex post-disposal device, modified and supplemented with this analysis, integrated the semi-dry reactor and the bag filter in a single body, so it follows that the improvement can make the device compact, the installation area, the operation fee, and management more convenient.

• Proceedings of the KSAR Conference
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• 2000.10a
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• pp.10-12
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• 2000

Members of the glycoprotein family, which includes CG, LH, FSH and TSH, comprise two noncovalently linked $\alpha$- and $\beta$-subunits. Equine chorionic gonadotropin (eCG), known as PMSG, has a number of interesting and unique characteristics since it appears to be a single molecule that possesses both LH- and FSH-like activities in other species than the horse. This dual activity of eCG in heterologous species is of fundamental interest to the study of the structure-function relationships of gonadotropins and their receptors. CG and LH $\beta$ genes are different in primates. In horse, however, a single gene encodes both eCG and eLH $\beta$-subunits. The subunit mRNA levels seem to be independently regulated and their imbalance may account for differences in the quantities of $\alpha$ - and $\beta$ -subunits in the placenta and pituitary. The dual activities of eCG could be separated by removal of the N-linked oligosaccharide on the $\alpha$-subunit Asn 56 or CTP-associated O-linked oligosaccharides. The tethered-eCG was. efficiently secreted and showed similar LH-like activity to the dimeric eCG. Interestingly, the FSH-like activity of the tethered-eCG was increased markedly in comparison with the native and wild type eCG. These results also suggest that this molecular can implay particular models of FSH-like activity not LH-like activity in the eCG/indicate that the constructs of tethered molecule will be useful in the study of mutants that affect subunit association and/or secretion. A single-chain analog can also be constructed to include additional hormone-specific bioactive generating potentially efficacious compounds that have only FSH-like activity. The LH/CG receptor (LH/CGR), a membrane glycoprotein that is present on testicular Leydig cells and ovarian theca, granulosa, luteal, and interstitial cells, plays a pivotal role in the regulation of gonadal development and function in males as well as in nonpregnant and pregnant females. The LH/CGR is a member of the family of G protein-coupled receptors and its structure is predicted to consist of a large extracellular domain connected to a bundle of seven membrane-spanning a-helices. The LH/CGR phosphorylation can be induced with a phorbol ester, but not with a calcium ionophore. The truncated form of LHR also was down-regulated normally in response to hCG stimulation. In contrast, the cell lines expressing LHR-t63I or LHR-628, the two phosphorylation-negative receptor mutant, showed a delay in the early phase of hCG-induced desensitization, a complete loss of PMA-induced desensitization, and an increase in the rate of hCG-induced receptor down-regulation. These results clearly show that residues 632-653 in the C-terminal tail of the LHR are involved in PMA-induced desensitization, hCG-induced desensitization, and hCG-induced down-regulation. Recently, constitutively activating mutations of the receptor have been identified that are associated with familial male-precocious puberty. Cells expressing LHR-D556Y bind hCG with normal affinity, exhibit a 25-fold increase in basal cAMP and respond to hCG with a normal increase in cAMP accumulation. This mutation enhances the internalization of the free and agonist-occupied receptors ~2- and ~17-fold, respectively. We conclude that the state of activation of the LHR can modulate its basal and/or agonist-stimulated internalization. Since the internalization of hCG is involved in the termination of hCG actions, we suggest that the lack of responsiveness detected in cells expressing LHR-L435R is due to the fast rate of internalization of the bound hCG. This statement is supported by the finding that hCG responsiveness is restored when the cells are lysed and signal transduction is measured in a subcellular fraction (membranes) that cannot internalize the bound hormone.

• Journal of the Korean Society of Marine Environment & Safety
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• v.22 no.6
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• pp.708-722
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• 2016

Land-Ocean Interactions in the Coastal Zone (LOICZ) models for nutrient budgets were used to estimate the seasonal capacity of the Youngsan Estuary and Youngam-Geumho Estuary to sink and/or supply nutrients such as dissolved inorganic phosphorus (DIP) and nitrogen (DIN) to provide an understanding of the behavior of the coupled biogeochemical cycles of phosphorus and nitrogen in the estuaries (Youngsan Estuary, Youngam-Geumho Estuary) near Mokpo Harbor. During non-stratified periods (May, September, and November, 2008), simple three-box models were applied in each sub-region of the system, while a two-layer box model was applied during on-site observation of stratification development (July, 2008). The resulting mass-balance calculation indicated that even after large discharges from artificial lakes (in May and July), DIP influxes due to a mixing exchange ($V_{X-3}$, or $V_{deep}$) were more than terrigenous loads, indicating the backward transportation of nutrients from a marine source. The model results also indicated that for nutrient loads (DIP and DIN fluxes) in September, an extreme congestion of nutrients occurred around the mouths (sub-region III of the model) of the estuaries, possibly due to an imbalance in physical circulations between the estuaries and offshore locations. In November, the Youngam-Geumho Estuary, into which freshwater was discharged from artificial lakes (Youngam and Geumho Lake), showed nutrient enrichment in the water column, but the Youngsan Estuary showed nutrient depletion. In conclusion, to efficiently control water quality in the estuaries near Mokpo Harbor, integrated environmental management programs should be implemented. I.e., the reduction of nutrient loads from land basins as well as the deposit of nutrient loads into adjacent coastal lines.

• Proceedings of the Korea Association of Crystal Growth Conference
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• 1996.06a
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• pp.179-200
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• 1996

The intrinsic instabilities of fluid flow occurred in the melt of the Czochralski crystal growth system Czochralski method, asymmetric flow patterns and temperature profiles in the melt have been studied by many researchers. The idea that the non-symmetric structure of the growing equipment is responsible for the asymmetric profiles is usually accepted at the first time. However further researches revealed that some intrinsic instabilities not related to the non-symmetric equipment structure in the melt could also appear. Ristorcelli had pointed out that there are many possible causes of instabilities in the melt. The instabilities appears because of the coupling effects of fluid flow and temperature profiles in the melt. Among the instabilities, the B nard type instabilities with no or low crucible rotation rates are analyzed by the visualizing experiments using X-ray radiography and the 3-D numerical simulation in this study. The velocity profiles in the Silicon melt at different crucible rotation rates were measured using X-ray radiography method using tungsten tracers in the melt. The results showed that there exits two types of fluid flow mode. One is axisymmetric flow, the other is asymmetric flow. In the axisymmetric flow, the trajectory of the tracers show torus pattern. However, more exact measurement of the axisymmetrc case shows that this flow field has small non-axisymmetric components of the velocity. When fluid flow is asymmetric, the tracers show random motion from the fixed view point. On the other hand, when the observer rotates to the same velocity of the crucible, the trajectory of the tracer show a rotating motion, the center of the motion is not same the center of the melt. The temperature of a point in the melt were measured using thermocouples with different rotating rates. Measured temperatures oscillated. Such kind of oscillations are also measured by the other researchers. The behavior of temperature oscillations were quite different between at low rotations and at high rotations. Above experimental results means that the fluid flow and temperature profiles in the melt is not symmetric, and then the mode of the asymmetric is changed when rotation rates are changed. To compare with these experimental results, the fluid flow and temperature profiles at no rotation and 8 rpm of crucible rotation rates on the same size of crucible is calculated using a 3-dimensional numerical simulation. A finite different method is adopted for this simulation. 50×30×30 grids are used. The numerical simulation also showed that the velocity and flow profiles are changed when rotation rates change. Futhermore, the flow patterns and temperature profiles of both cases are not axisymmetric even though axisymmetric boundary conditions are used. Several cells appear at no rotation. The cells are formed by the unstable vertical temperature profiles (upper region is colder than lower part) beneath the free surface of the melt. When the temperature profile is combined with density difference (Rayleigh-B nard instability) or surface tension difference (Marangoni-B nard instability) on temperature, cell structures are naturally formed. Both sources of instabilities are coupled to the cell structures in the melt of the Czochralski process. With high rotation rates, the shape of the fluid field is changed to another type of asymmetric profile. Because of the velocity profile, isothermal lines on the plane vertical to the centerline change to elliptic. When the velocity profiles are plotted at the rotating view point, two vortices appear at the both sides of centerline. These vortices seem to be the main reason of the tracer behavior shown in the asymmetric velocity experiment. This profile is quite similar to the profiles created by the baroclinic instability on the rotating annulus. The temperature profiles obtained from the numerical calculations and Fourier transforms of it are quite similar to the results of the experiment. bove esults intend that at least two types of intrinsic instabilities can occur in the melt of Czochralski growing systems. Because the instabilities cause temperature fluctuations in the melt and near the crystal-melt interface, some defects may be generated by them. When the crucible size becomes large, the intensity of the instabilities should increase. Therefore, to produce large single crystals with good quality, the behavior of the intrinsic instabilities in the melt as well as the effects of the instabilities on the defects in the ingot should be studied. As one of the cause of the defects in the large diameter Silicon single crystal grown by the

• The Journal of Korean Institute of Communications and Information Sciences
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• v.13 no.6
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• pp.521-528
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• 1988

Into the telecommunications industry, which had been monopolistic, a few advanced countries introduced competition through 70's and 80's. And this trend is going on worldwide. The introduction of competition into the industry is made mainly in the long distance, international and enhanced market. This liberalisation results from the fundamental change of the cost function. Suggesting that the cost comprises of that of the facility sector and that of the operation sector there exists the economies of scale in the facility sector in general. The major ground for the monopolistic industrial structure in the past was the natural monopoly depending on the economies of scale. But the rapid advance of the technology by a large margin. This decrease has resulted in the change of the cost function. That is while there exists the economies of scale in the smaller production scale, the average cost increases beyond a certain scale. This means that the natural monopoly collapsed, and that the competitive structure is more efficient than the monopolistic structure. But, because there exists economies of scale in the smaller scale, the desirable number of players, which could result in efficient industry structure depends on the market size. Such correlation between technological level market size and the degree of regulation is found in the case of U.S.A., Japan and U.K., where deregulation policy of the telecommunications market has already been carried out. In U.S.A., which has the largest market and the highest technological level the degree of regulation is lowest. Also in the order of Japan and U.K. the regulation is severer. Japan and U.K. are likely to liberalize still more, as the technology advances and the market grows. This article is just the beginning of the research, and this hypothesis requires more detailed research.

• Korean Journal of Animal Reproduction
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• v.24 no.4
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• pp.357-364
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• 2000

Members of the glycoprotein family, which includes CG, LH, FSH and TSH, comprise two noncovalently linked $\alpha$- and $\beta$-subunits. Equine chorionic gonadotropin (eCG), known as PMSG, has a number of interesting and unique characteristics since it appears to be a single molecule that possesses both LH- and FSH-like activities in other species than the horse. This dual activity of eCG in heterologous species is of fundamental interest to the study of the structure-function relationships of gonadotropins and their receptors. CG and LH $\beta$ genes are different in primates. In horse, however, a single gene encodes both eCG and eLH $\beta$ -subunits. The subunit mRNA levels seem to be independently regulated and their imbalance may account for differences in the quantities of $\alpha$ - and $\beta$-subunits in the placenta and pituitary. The dual activities of eCG could be separated by removal of the N-linked oligosaccharide on the $\alpha$-subunit Asn 56 or CTP-associated O-linked oligosaccharides. The tethered-eCG was efficiently secreted and showed similar LH-like activity to the dimeric eCG. Interestingly, the FSH-like activity of the tethered-eCG was increased markedly in comparison with the native and wild type eCG. These results also suggest that this molecular can implay particular models of FSH-like activity not LH-like activity in the eCG/indicate that the constructs of tethered molecule will be useful in the study of mutants that affect subunit association and/or secretion. A single-chain analog can also be constructed to include additional hormone-specific bioactive generating potentially efficacious compounds that have only FSH-like activity. The LH/CG receptor (LH/CGR), a membrane glycoprotein that is present on testicular Leydig cells and ovarian theca, granulosa, luteal, and interstitial cells, plays a pivotal role in the regulation of gonadal development and function in males as well as in nonpregnant and pregnant females. The LH/CGR is a member of the family of G protein-coupled receptors and its structure is predicted to of a large extracellular domain connected to a bundle of seven membrane-spanning a-helices. The LH/CGR phosphorylation can be induced with a phorbol ester, but not with a calcium ionophore. The truncated form of LHR also was down-regulated normally in response to hCG stimulation. In contrast, the cell lines expressing LHR-t631 or LHR-628, the two phosphorylation-negative receptor mutant, showed a delay in the early phase of hCG-induced desensitization, a complete loss of PMA-induced desensitization, and an increase in the rate of hCG-induced receptor down-regulation. These results clearly show that residues 632~653 in the C-terminal tail of the LHR are involved in PMA-induced desensitization, hCG-induced desensitization, and hCG-induced down-regulation. Recently, constitutively activating mutations of the receptor have been identified that are associated with familial male-precocious puberty. Cells expressing LHR-D556Y bind hCG with normal affinity, exhibit a 25-fold increase in basal cAMP and respond to hCG with a normal increase in cAMP accumulation. This mutation enhances the internalization of the free and agoinst-occupied receptors ~2- and ~17- fold, respectively. We conclude that the state of activation of the LHR can modulate its basal and/or agonist-stimulated internalization. Since the internalization of hCG is involved in the termination of hCG actions, we suggest that the lack of responsiveness detected in cells expressing LHR-L435R is due to the fast rate of internalization of the bound hCG. This statement is supported by the finding that hCG responsiveness is restored when the cells are lysed and signal transduction is measured in a subcellular fraction (membranes) that cannot internalize the bound hormone.