• The Korean Journal of Pesticide Science
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• v.11 no.3
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• pp.131-137
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• 2007

CoMFA and CoMSIA model were derived and reviewed on the insecticidal activities of N-substituents (X) on the imidazol ring in imidacloprid analogues at the different alignment condition. Regarding the predictability ($q^2$ or $r_{cv.}^2$) and fitness ($r_{ncv.}^2$) of the two optimized models, the atom based fit (A) alignments were better than that of the field fit (F) alignment and, on the other hand, CoMSIA (A10) model was better than CoMFA (A5) model. Also, from the most optimized CoMSIA (A10) model, the insecticidal activity by N-substituents (X) was dependence on the electrostatic field and H-bond acceptor field. It is predicted that, from the contour maps with optimized CoMSIA (A10) model, H-bond acceptors at ortho- and meta- position will contribute for improving of insecticidal activities and, as the functional groups of carbonyl oxygen atom are charged negatively and positively charged at the ortho- position of benzyl group, insecticidal activities will also be improved.

• Journal of the Korean Applied Science and Technology
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• v.38 no.4
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• pp.1003-1009
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• 2021

A study on the associative properties of sodium hyaluronate (NaHA) and Alkane-bis (dimethylalkylammonium bromide) surfactants in aqueous solution was investigated in relation to the chemical structure of surfactants. As a result of measuring the interfacial tension, a parabolic graph showing the minimum value (c_min) at a specific concentration was shown. Above this minimum concentration the increase in interfacial tension is thought to be related to the formation of aggregates of NaHA chains and dimeric surfactants. The plot of viscosity vs surfactant concentration shows a slight maxium at c_min and a viscosity decrease at high surfactant concentrations. Viscosity nonlinear behavior is related to the size increase due to the complex growth and to the size shrinkage following from the interaction with electrolyte ions and free micelles. The results of surface tension measurements show a broad region of surface tension decrease, indicating the NaHA-surfactant interaction. The increase in surface tension above c_min may be related to the adsorption of clusters, consisting of free NaHA chains and dimeric surfactant. The strong adsorption of surfactant is observed at high concentrations.

• The Korean Journal of Pharmacology
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• v.24 no.1
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• pp.17-29
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• 1988

The author examined the effects of lidocaine on the veratrine-or potassium-induced release of neurotransmitters to determine the possible role of amino acid neurotransmitters in lidocaine-induced convulsion. The examined transmitters were gamma-aminobutyric acid (GABA), aspartic acid, glutamic acid and norepinephrine which are released from the synaptosomes. Furthermore, the effects of lidocaine on the binding to receptors and synaptosomal uptake of the two transmitters, GABA and glutamic acid, were determined in crude synaptic membranes and synaptosomes. In addition, the effects of propranolol, norepinephrine and serotonin on the release of amino acid neurotransmitters were also examined. The veratrine-induced release of GABA was most severely inhibited by lidocaine and propranolol, while norepinephrine and serotonin reduced the release of aspartic acid and glutamic acid more than the GABA release. Generally the potassium-induced release was much more resistant to the lidocaine action than the veratrine-induced release. Among the neurotransmitters examined, the aspartic acid release was most prone to the lidocaine action, while the GABA release was most resistant. Concentrations of lidocaine below 1 mM did not significantly change the GABA and glutamic acid receptor binding and uptake. These results indicate that the blocking of sodium channels by lidocaine can result in the selective depression of the GABA release. This may result in unlimited excitation of the central nervous system.

• Journal of the Korean Chemical Society
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• v.41 no.6
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• pp.277-283
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• 1997

Platinum(II) complexes(where, $[Pt(L)_2X_2]$; L=isoxazole(isox), 3,5-dimethylisoxazole(3,5-diMeisox), 3-methyl,5-phenylisoxazole(3-Me,5-Phisox), and 4-amino-3,5-dimethylisoxazole(4-ADI); X=Cl, Br) with planar ligands are investigated on antitumor activity by MM2 and EHMO calculations. It was found that, the net atomic charges of the halogen atoms in all of cis-, trans-isomers are greater than that of the nitrogen with planar form, indicating that ionic character of Pt-X bond is greater than that of Pt-N. Also, the ${\sigma}MO$ energy level($E{\sigma}_{(Pt-X)}$) of the interaction between $d_{x2-y2}$ orbital of Pt atom and $p_x$ orbital of X found to be higher than that of between $d_{x2-y2}$ orbital of Pt atom and $p_x$ orbital of N about all the complexes. It is found that bond strength of between Pt and X atom is weaker than that of between Pt and N atom. The ${\sigma}MO$ energy level($E{\sigma}_{(Pt-X)}$) of trans- complexes found to be higher than that of cis- complexes, as a result of bond strength of Pt-X in cis- and trans-complexes, for all the complexes. The degree of dissociation of X atom in Pt-X bond for trans-complexes are related to antitumor activity and the logIA value of inhibitory activity coefficient(IA).

• The Korean Journal of Nuclear Medicine
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• v.31 no.4
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• pp.421-426
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• 1997

We evaluated the in vivo kinetics, distribution, and pharmacology of N-(4-[$^{18}F$]fluoromethylbenzyl)spiperone ([$^{18}F$]FMBS), a newly developed derivative of spiperone, as a potentially more selective radiotracer for the dopamine (DA) $D_2$ receptors. Mice received 1.9-3.7 MBq (1.8-3.6 nmol/kg) of [$^{18}F$]FMBS by tail vein injection. The time course and regional distribution of the tracer in brain were assessed. Blocking studies were carried out by intravenously preinjecting DA $D_2$ receptor blockers (spiperone, butaclamol) as well as drugs with high affinity for DA $D_1$ (SCH 23390), DA transporter (GBR 12909), and serotonin $S_2$ ($5-HT_2$) (ketanserin) sites. After injection of the tracer, the radioactivity in striatum increased steadily over time, resulting in a striatal-to-cerebellar ratio of 4.8 at 120 min postinjection. By contrast, the radioactivity in cerebellum, frontal cortex, and remaining cortex washed out rapidly. Preinjection of unlabeled FMBS (1 mg/kg) and spiperone (1 mg/kg) reduced [$^{18}F$]FMBS striatal-to-cerebellar ratio by 41% and 80%, respectively. (+)-Butaclamol (1 mg/kg) blocked 80% of the striatal [$^{18}F$]FMBS binding, while (-)-butaclamol (1 mg/kg) did not. Preinjection of SCH 23390 (1 mg/kg) and GBR 12909 (5 mg/kg) had no significant effect on [$^{18}F$]FMBS binding. Ketanserin (1 mg/kg), a ligand for the $5-HT_2$ receptors, did not cause significant inhibition either in striatum, in frontal cortex, or the remaining cortex. The results demonstrate that [$^{18}F$]FMBS labels DA $D_2$ receptors selectively in vivo in the mouse brain. It may hold promise as a selective radiotracer for studying DA $D_2$ receptors in vivo by PET.

• Journal of the Korean Chemical Society
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• v.43 no.4
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• pp.461-468
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• 1999

Acetolactate synthase (ALS) catalyzes the first common reaction in the biosynthesis of branched-chain amino acids, valine, leucine, and isoleucine. ALS is the common target of several classes of structurally diverse herbicides, the triazolopyrimidines, the imidazolinones, the sulfonylureas, and pyrimidyl-oxy-benzoates. We examined ihibitory activities of newly synthesized triazolopyrimidine sulfonamide derivatives using partially purified ALS from barley. $IC_{50}$ values for the active derivatives are 0.5nM∼8$\mu$M. Among them TP1 and TP2 are the most potent ALS inhibitors with $IC_{50}$ values of 0.5nM and 1.6nM, respectively. These inhibitors are more potent in the inhibition of barley ALS than commercial herbicides, Metosulam ($IC_{50}$;3.6 nM), Flumetsulam ($IC_{50}$;126 nM), and Cadre ($IC_{50};4 {\mu}M$). The progress curves for inhibition of ALS by TP2 showed that the amount of inhibition increases with time. The inhibition of ALS by TP2 was mixed-type inhibition with respect to pyruvate. Dual inhibition analyses of TP2 versus an imidazolinone, Cadre, and Leu showed parallel and intercepting kinetic pattern, respectively. The results suggest that TP2 binds to ALS competively with Cadre but not with Leu. Chemical modification of cysteinly residues in ALS decreased the sensitivity of ALS to Leu, while the modification did not affect the sensitivity of ALS to TP2 and Cadre.

• Journal of Life Science
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• v.33 no.11
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• pp.950-955
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• 2023

Cell division is an essential process for the survival and development of living organisms. It is critical that duplicated chromosomes are properly segregated into daughter cells during mitosis. The centrosome is the core organelle that forms the microtubule-organizing center (MTOC), which generates the microtubules that make up the mitotic spindle during cell division. The centrosome is also involved in cell signaling and motility. In normal cells, there is one centrosome in G1 that replicates into two in the S phase and matures through G2. During the M phase, duplicated centrosomes move to both ends of the cell, and spindle microtubules that are generated from MTOC move the chromosome to both ends. The cells then split into two to complete the cell division. However, a phenomenon called centrosome amplification (CA), in which the number of centrosomes is higher than normal, is common in cancer cells and can lead to chromosome instability (CIN). This paper discusses the process of centrosome replication and the role of PLK4 in this process. The possible consequences of centrosome amplification and how the PLK4 inhibitor may be able to treat certain types of cancer cells, such as breast cancer and neuroblastoma, will also be discussed.

• Journal of Life Science
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• v.25 no.5
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• pp.594-600
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• 2015

Protein-protein interactions have a critical role in the regulation of many cellular functions. Postsynaptic density-95/disks large/zonula occludens-1 (PDZ) domain is one of domains that mediate protein-protein interactions. PDZ domains typically bind to the specific motif at the carboxyl (C)-terminal end of partner proteins. Multi-PDZ domain protein 1 (MUPP1), which has 13 PDZ domains, serves a scaffolding function for structure proteins and signaling proteins, but the cellular function of MUPP1 has not been fully elucidated. We used the yeast two-hybrid system to identify proteins that interact with PDZ domains of MUPP1. We found an interaction between MUPP1 and muskelin. Muskelin was recently identified as a GABA_A receptor (GABA_AR) α1 subunit binding protein and known to have a role in receptor endocytosis and degradation. Muskelin bound to the 3^rd PDZ domain, but not to other PDZ domains of MUPP1. The C-terminal end of muskelin was essential for the interaction with MUPP1 in the yeast two-hybrid assay. When co-expressed in HEK-293T cells, muskelin but not the C-terminal deleted muskelin was co-immunoprecipitated with MUPP1. In addition, MUPP1 co-localized with muskelin at the same subcellular region in cells. These findings collectively suggest that MUPP1 or its interacting proteins could modulate GABA_AR trafficking and turnover through the interaction with muskelin.

• Journal of the Korean Chemical Society
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• v.33 no.2
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• pp.156-163
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• 1989

The $ν_a+amide II$ combination band of thiopropionamide has been recorded for investigation of Hydrogen bonding between thiopropionamide (TPA) and N,N-dimethylalkylamide (DMF, DMA and DMP) in carbon tetrachloride over the range of $5^{\circ}$ to $55^{\circ}$. The combination band of monomeric TPA and hydrogen-bonded TPA can be resolved by Lorentzian-Gaussian product function into monomeric TPA and hydrogen-bonded TPA with amides. The association constants ($K_1$) for the hydrogen-bonded TPA were calculated by the concentrations of the monomeric TPA and the hydrogen-bonded TPA obtained from the computer resolved absorption bands. Thermodynamic parameters for the Hydrogen bonding have been evaluated by the analysis of the temperature dependent spectra. The ${\Delta}$$H^{\circ}$ of hydrogen-bonded TPA with DMF, DMA and DMP have been found to be-12.5, -13.5 and -14.1 kJ/mol, respectively. The corresponding ${\Delta}$$S^{\circ}$for the above system were -15.2, -17.9 and -22.3 J/mol${\cdot}$deg, respectively.

• Transactions of the Korean Society of Mechanical Engineers
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• v.14 no.1
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• pp.54-71
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• 1990

The fabrication of ceramic machine components by injection molding(CIM : Ceramic Injection Molding) is critically dependent on the shaping and binder extraction techniques. Injection molding is of keen interest to ceramic industries because CIM is suitable for making an intricate shape and manufacturing cost is lower than other process when production scale is large. The success of the molding process is dependent on the correct formulation of the organic vehicle and the achievement of optimum filler loading. Fine alumina powders and polyethylene binder systems were employed to prepare moldable blend then produce a simple specimen by compression molding. Flow characteristics of the mixture was evaluated by viscosity measurement. Optimum binder system and ceramic volume loading for injection molding were determind. A good debinding technique was utilized to improve the quality of debinded parts and save the debinding time. The simple ceramic part was successfully sintered after debinding and its microstructure examined with SEM revealed good consolidation.