• Molecules and Cells
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• v.41 no.6
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• pp.545-552
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• 2018

Spleen tyrosine kinase (SYK) is a cytosolic non-receptor protein tyrosine kinase. Because SYK mediates key receptor signaling pathways involving the B cell receptor and Fc receptors, SYK is an attractive target for autoimmune disease and cancer treatments. To date, representative oral SYK inhibitors, including fostamatinib (R406 or R788), entospletinib (GS-9973), cerdulatinib (PRT062070), and TAK-659, have been assessed in clinical trials. Here, we report the crystal structures of SYK in complex with two newly developed inhibitors possessing 4-aminopyrido[4,3-D]pyrimidine moieties (SKI-G-618 and SKI-O-85). One SYK inhibitor (SKI-G-618) exhibited moderate inhibitory activity against SYK, whereas the other inhibitor (SKI-O-85) exhibited a low inhibitory profile against SYK. Binding mode analysis indicates that a highly potent SYK inhibitor might be developed by modifying and optimizing the functional groups that interact with Leu377, Gly378, and Val385 in the G-loop and the nearby region in SYK. In agreement with our structural analysis, one of our SYK inhibitor (SKI-G-618) shows strong inhibitory activities on the ${\beta}$-hexosaminidase release and phosphorylation of SYK/Vav in RBL-2H3 cells. Taken together, our findings have important implications for the design of high affinity SYK inhibitors.

• The KIPS Transactions:PartD
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• v.13D no.3 s.106
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• pp.317-324
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• 2006

In this paper, we propose a new indexing technique to solve various queries which have a strong good point not only database indexing schema take advantage of converting from semi-structured data to structured data but also performance is more faster than before. We represent structure information of XML document between nodes of tree that additional numbering information which can be bit-stream without modified structure of XML tree. And, We add in indexing schema searching incidental structure information in the process. In Querying schema, we recover ancestor nodes through give information of node using indexing schema in complete path query expression as well as relative path query expression. Therefore, it takes advantage of making derivative query expression with given query. In this process, we recognize that indexing and querying schema can get searched result set faster and more accurate. Because response time is become shorter by bit operating, when query occur and it just needs information of record set earch node in database.

• Korean Journal of Food Science and Technology
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• v.6 no.1
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• pp.6-11
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• 1974

Four new compounds; 2,2'-methylene-bis [3, 4, 6-trichloro ${{\beta}-(o-nitroanilino)$ propionoxy} benzene]; m.p. $200{\sim}202^{\circ}C,\;C_{31}H_{22}O_8N_4Cl_6$ 2,2'-methylene-bis [3, 4, 6-trichloro ${{\beta}-(p-nitroanilino)$ propionoxy} benzene]; m.p. $168-170^{\circ}C,\;C_{31}H_{22}O_8N_4Cl_6$ : 2,2'-Methylene-bis [3, 4, 6-trichloro ${{\beta}-(o-chloro-p-nitroanilino)$ propionoxy} benzene]; m.p. $170.5-172.5^{\circ}C,\;C_{31}H_{20}O_8N_4Cl_8$ : 2,2'-Methylene-bis [3, 4, 6-trichloro ${{\beta}-(c-methyl-p-nitroanilino)$ propionoxy} benzene]; m.p. $163-164^{\circ}C,\;C_{33}H_{26}O_8N_4Cl_6$-were synthesized by Mannich reaction from 2,2'-Methylene-bis (3, 4, 6-trichloroacetoxy benzene) and their antimicrobial activities against the microorganisms Staphylococcus aureus, Escherichia coli, Bacillus subtilis Natto, Brevibacterium ammoniagenes, Candida tropicalis, Rhodotorula glutinis, Pseudomonas ovalis, Aspergillus candidus Link, Aspergillus awamori Nakazawa. Aspergillus niger var. Tieghem, Aspergillus usami Sakakuchi, Penicillium notatum-were tested. 2,2'-methylene-bis [3, 4, 6-trichloro ${{\beta}-(o-nitroanilino)$ propionoxy} benzene] showed a strong antimicrobial activity against Bacilus subtilis Natto and Brevibacterium ammoniagenes.

• Analytical Science and Technology
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• v.20 no.5
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• pp.400-405
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• 2007

The comparative analysis of glycerin in cosmetic samples was carried out by LC/MS and $^1H$ NMR spectrometry. For the LC/MS analysis, aqueous solution was controlled in strong basic condition with sodium hydroxide, and benzoyl chloride was added to the solution for the derivatization of glycerin. The derivative was extracted using pentane and analyzed by the LC/MS. For the $^1H$ NMR analysis, sample was directly dissolved in $D_2O$ solvent without pretreatment. The quantitative analysis of glycerin was done by $^1H$ NMR ERETIC method. The analysis results of LC/MS and $^1H$ NMR showed that the calibration curves were a good linearity with $r^2=0.9991$ in the range of 0.1 to $10{\mu}g/mL$ and $r^2=1$ in the range of 25 to $500{\mu}g/mL$, respectively.

• Analytical Science and Technology
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• v.20 no.3
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• pp.198-203
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• 2007

The analysis method of 3-Monochloropropane-1,2-diol (3-MCPD) compound in water was developed using liquid chromatography with mass spectrometric detection. Aqueous solution was controlled in strong basic condition with sodium hydroxide, and then $25{\mu}L$ of benzoyl chloride was added to the solution for the derivatization of 3-MCPD. The derivative was extracted using pentane and analyzed by the selected ion monitoring (SIM) method of LC-MS. The results of analyses showed that the calibration curves was in the range of 1.0 to $100{\mu}g/mL$ with a good linearity (correlation coefficient of $r^2=0.992$) and limit of detection was below $0.01{\mu}g/mL$. The recoveries of this analysis method by LC-MS were 92.3-98.0 %.

• Textile Coloration and Finishing
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• v.35 no.4
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• pp.214-220
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• 2023

Poly(vinyl alcohol) (PVA) is a common hydrophilic polymer that is synthesized through the saponification reaction of poly(vinyl ester)-based polymers, mostly using poly(vinyl acetate) (PVAc) as a precursor. The heterogeneous saponification reaction of poly(vinyl ester)-based films leads to PVA films with new surface properties. Cellulose acetate (CA), in which the hydroxyl group of cellulose is replaced by an acetyl group, is a typical cellulose derivative capable of overcoming the low processability of cellulose due to strong hydrogen bonding. In this study, P(VAc/VPi)/CA blended films were prepared by the solvent casting, and then PVA/Cellulose blended films with improved surface properties were prepared by heterogeneous saponification. The structural changes caused by heterogeneous saponification were confirmed by FT-IR analysis, where both saponification and deacetylation reactions occurred in the saponification solution. In addition, the surface property changes were analyzed by FE-SEM and contact angle analyses, and the transmittance changes of the modified films were also assessed.

• Journal of Advanced Marine Engineering and Technology
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• v.39 no.6
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• pp.633-641
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• 2015

Several complex processes that are employed in industries, such as shipping, power plants, and the petrochemical industry, involve time-varying behavior as well as strong nonlinear behavior during operation. The fixed-parameter proportional-integral-derivative (PID) controllers have difficulty in dealing with control problems that occur in such processes. In this paper, we propose a method of designing a nonlinear PID controller for industrial processes that exhibit a large number of nonlinearities and time-varying behavior. The gains of the nonlinear PID controller are characterized by a simple nonlinear function of the error and/or error rate depending on the process set-point and output. We tune the user-defined parameters using a genetic algorithm by minimizing the integral of time absolute error (ITAE) index. We verify the effectiveness of the proposed method by performing a comparison of the proposed method and two other nonlinear and adaptive methods that are employed for reference tracking, disturbance-rejection performances, and robustness to parameter changes on a continuously stirred tank reactor.

• The Korean Journal of Mycology
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• v.13 no.4
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• pp.203-212
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• 1985

Of 450 strains isolated from the soil microbes collected in various locations in Korea, a strain had a strong inhibitory activity against bacterial ${\alpha}-amylase$ and was named strain DMC-72 of the genus Streptomyces. The amylase inhibitory metabolite produced by this strain was purified by means of acetone precipitation, adsorption on Amberlite IRC-50 and SP-Sephadex C-25. The inhibitor was found to be a derivative of oligosaccharides by spectral and chemical data. The inhibitor was stable at the pH range of $1{\sim}13$ and at $100^{\circ}C$ for half an hour, also inhibited other amylases such as salivary ${\alpha}-amylase$, pancreatic ${\alpha}-amylase$, fungal ${\alpha}-amylase$ and glucoamylase. However, it showed no inhibitory activity against ${\alpha}-glucosidase$, ${\beta}-glucosidase$, dextranase, and ${\beta}-amylase$. The kinetic studies of the inhibitor showed that its inhibitory effects on starch hydrolysis by ${\alpha}-amylase$ were noncompetitive.

• Ecology and Resilient Infrastructure
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• v.4 no.3
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• pp.130-141
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• 2017

We evaluated the field application feasibility that biologically derived substances (Naphthoquinone derivate: NQ 2-0) can be used for the eco-friendly mitigation of natural harmful cyanobacterial blooms in freshwater. We conducted a 30 ton scale mesocosm experiment to investigate the effects of NQ 2-0 on biotic and abiotic factors in water collected from Gi-heung reservoir. In the mesocosm experiments, the abundance of Microcystis sp. was continuously increased in the control. However, the Microcystis sp. cell density was sharply decreased on the $10^{th}$ day. In the treatment, NQ 2-0 showed the strong and selective algicidal activity toward the target cyanobacteria (Microcystis sp.). Accordingly, the algicidal activity of NQ 2-0 compound increased gradually until $10^{th}$, $15^{th}$ days and algal biomass was decreased to 99.4 and 100 %, respectively. NQ 2-0 compound was not only selective algicidal activity but also the growth of other phytoplankton and increased the Shannon-Wiener diversity index of phytoplankton. In the mesocosm experiments, the dynamics of biotic (bacteria, heterotrophic nanoflagellate, ciliates, zooplankton) and abiotic (water temperature, dissolved oxygen, pH, conductivity, nutrients) factors remained unaffected. These results suggest that NQ 2-0 could be a selective and ecologically safe algicide to mitigate harmful cyanobacterial blooms. In addition, it is believed that NQ 2-0 will play a major role in forming a healthy aquatic ecosystem by facilitating habitat and food supply of aquatic organisms.

• Journal of Microbiology and Biotechnology
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• v.23 no.5
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• pp.644-651
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• 2013

The fermented manure derivative known as Preparation 500 is traditionally used as a field spray in biodynamic agriculture for maintaining and increasing soil fertility. This work aimed at characterizing the product from a microbiological standpoint and at assaying its bioactive properties. The approach involved molecular taxonomical characterization of the culturable microbial community; ARISA fingerprints of the total bacteria and fungal communities; chemical elemental macronutrient analysis via a combustion analyzer; activity assays for six key enzymes; bioassays for bacterial quorum sensing and chitolipooligosaccharide production; and plant hormone-like activity. The material was found to harbor a bacterial community of $2.38{\times}10^8$ CFU/g dw dominated by Gram-positives with minor instances of Actinobacteria and Gammaproteobacteria. ARISA showed a coherence of bacterial assemblages in different preparation lots of the same year in spite of geographic origin. Enzymatic activities showed elevated values of ${\beta}$-glucosidase, alkaline phosphatase, chitinase, and esterase. The preparation had no quorum sensing-detectable signal, and no rhizobial nod gene-inducing properties, but displayed a strong auxin-like effect on plants. Enzymatic analyses indicated a bioactive potential in the fertility and nutrient cycling contexts. The IAA activity and microbial degradation products qualify for a possible activity as soil biostimulants. Quantitative details and possible modes of action are discussed.