• 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.

• Applied Biological Chemistry
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• v.40 no.5
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• pp.442-446
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• 1997

A new analytical method was developed by HPLC after supercritical fluid extraction and fluorogenic derivatization for the determination of quinclorac (3,7-dichloro-8-quinoline carboxylic acid) in soil. The graminicide quinclorac was extracted from soil by supercritical fluid extraction. Supercritical carbon dioxide at 7000 psi $(80^{\circ}C)$ modified with 30% of methanol extracted quinclorac from soil samples at the level of $0.1ng\;g^{-1}$ with 96% recovery. Extracted quinclorac was determined by HPLC as a fluorescent derivative. Derivatization was made with 4-bromomethyl-7-methoxycoumarin (4-Br-Mmc) using 18-crown-6-ether as a catalyst. The conversion was completed within 30 min and the limit of detection was 0.5 ppb to prove that the procedure could be used in the residue analysis of the pesticides containing carboxylic acid group.

• Journal of Korean Society on Water Environment
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• v.20 no.3
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• pp.281-289
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• 2004

Optimal analytical conditions have been established for mixing and reaction coil length, concentrations of ECR, CTAB, and acetate, reaction temperature and pH in the determination of aluminum by using flow injection analysis(FIA). Detection limit and repeatability for this system were $3{\mu}g/L$ and better than 1% of relative standard deviation, respectively. The interference from iron(III) was suppressed up to 6mg/L of iron(III) by $0.1{\mu}M$ ascorbic acid, and the interference from fluoride could be tolerated in absorption of Al/ECR/CTAB derivative by 10mM boric acid at pH 3.5 adjusted with nitric acid. This FIA system was applied to the determination of aluminum leached from cooking utensils by distilled and tap water containing fluoride ranged from 0.5 to 2mg/L by measurement of absorbance for Al/ECR/CTAB at 585nm. The leached aluminum content was increased with increasing concentration of fluoride. The aluminum contents leached from aluminum utensils by tap water were about 9 fold higher than those leached by distilled water, whereas aluminum contents leached by distilled water containing fluoride were about 2 fold higher compared to those leached by distilled water. That represented that other dissolved substances as well as fluoride in tap water contributed to liberation of aluminum from aluminum utensils. A comparison between FIA data and ICP-AES data by correlation and paired t test showed that the FIA system could be accepted as a good alternative method for the determination of aluminum in tap water.

• Journal of Korean Society on Water Environment
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• v.23 no.2
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• pp.236-243
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• 2007

Fluorescence measurements of dissolved organic matter (DOM) have the superior advantages over other analysis tools for the applications to water quality management due to their rapid analysis. It is known that protein-like fluorescence characteristics are well corelated with microbial activities and biodegradable organic matter. In this study, potential biochemical oxygen demand (BOD) predictor were explored using the fluorescence peak intensities and/or the integrated fluorescence intensities derived from synchronous fluorescence spectra and the first derivative spectra of river samples. A preliminary study was conducted using a mixture of a river and a treated sewage to test the feasibility of the approach. It was demonstrated that the better BOD predictor can be derived from synchronous fluorescence spectra and the derivatives when the difference between the emission and the excitation wavelengths (${\Delta}{\gamma}$) was large. The efficacy of several selected fluorescence parameters was rivers in Seoul. The fluorescence parameters exhibited relatively good correlation coefficients with the BOD values, ranging from 0.59 to 0.90. Two parameters were suggested to be the optimum BOD predictors, which were a fluorescence peak at a wavelength of 283 nm from the synchronous spectrum at the ${\Delta}{\gamma}$ value of 75 nm, and the integrated fluorescence intensity of the first derivatives of the spectra at the wavelength range between 245 nm and 280 nm. Each BOD predictor showed the correlation coefficients of 0.89 and 0.90, respectively. It is expected that the results of this study will provide important information to develop a real-time efficient sensor for river BOD in the future.

• Mycobiology
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• v.49 no.5
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• pp.491-497
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• 2021

An endolichenic fungus Xylaria grammica EL000614 produces grammicin, a potent nematicidal pyrone derivative that can serve as a new control option for root-knot nematodes. We optimized an Agrobacterium tumefaciens-mediated transformation (ATMT) protocol for X. grammica to support genetic studies. Transformants were successfully generated after co-cultivation of homogenized young mycelia of X. grammica with A. tumefaciens strain AGL-1 carrying a binary vector that contains the bacterial hygromycin B phosphotransferase (hph) gene and the eGFP gene in T-DNA. The resulting transformants were mitotically stable, and PCR analysis showed the integratin of both genes in the genome of transformants. Expression of eGFP was confirmed via fluorescence microscopy. Southern analysis showed that 131 (78.9%) out of 166 transformants contained a single T-DNA insertion. Crucial factors for producing predominantly single T-DNA transformants include 48 h of co-cultivation, pretreatment of A. tumefaciens cells with acetosyringone before co-cultivation, and using freshly prepared mycelia. The established ATMT protocol offers an efficient tool for random insertional mutagenesis and gene transfer in studying the biology and ecology of X. grammica.

• Journal of Microbiology and Biotechnology
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• v.31 no.9
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• pp.1191-1199
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• 2021

Enteropathogenic Escherichia coli (EPEC), which belongs to the attaching and effacing diarrheagenic E. coli strains, is a major causative agent of life-threatening diarrhea in infants in developing countries. Most EPEC isolates correspond to certain O serotypes; however, many strains are non-typeable. Two EPEC strains, EPEC001 and EPEC080, which could not be serotyped during routine detection, were isolated. In this study, we conducted an in-depth characterization of their putative O-antigen gene clusters (O-AGCs) and also performed constructed mutagenesis of the O-AGCs for functional analysis of O-antigen (OAg) synthesis. Sequence analysis revealed that the occurrence of O-AGCs in EPEC001 and E. coli O132 may be mediated by recombination between them, and EPEC080 and E. coli O2/O50 might acquire each O-AGC from uncommon ancestors. We also indicated that OAg-knockout bacteria were highly adhesive in vitro, except for the EPEC001 wzy derivative, whose adherent capability was less than that of its wild-type strain, providing direct evidence that OAg plays a key role in EPEC pathogenesis. Together, we identified two EPEC O serotypes in silico and experimentally, and we also studied the adherent capabilities of their OAgs, which highlighted the fundamental and pathogenic role of OAg in EPEC.

• Journal of Ginseng Research
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• v.43 no.4
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• pp.625-634
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• 2019

Background: Ginsenoside Rg3, a derivative of steroidal saponins abundant in ginseng, has a range of effects on cancer cells, including anti-cell proliferation and anti-inflammation activity. Here, we investigate two long noncoding RNAs (lncRNAs), STXBP5-AS1 and RFX3-AS1, which are hypomethylated and hypermethylated in the promoter region by Rg3 in MCF-7 cancer cells. Methods: The lncRNAs epigenetically regulated by Rg3 were mined using methylation array analysis. The effect of the lncRNAs on the apoptosis and proliferation of MCF-7 cells was monitored in the presence of Rg3 or Korean Red Ginseng (KRG) extract after deregulating the lncRNAs. The expression of the lncRNAs and their target genes was examined using qPCR and Western blot analysis. The association between the expression of the target genes and the survival rate of breast cancer patients was analyzed using the Kaplan-Meier Plotter platform. Results: STXBP5-AS1 and RFX3-AS1 exhibited anti- and pro-proliferation effects, respectively, in the cancer cells, and the effects of Rg3 and KRG extract on apoptosis and cell proliferation were weakened after deregulating the lncRNAs. Of the genes located close to STXBP5-AS1 and RFX3-AS1 on the chromosome, STXBP5, GRM1, RFX3, and SLC1A1 were regulated by the lncRNAs on the RNA and protein level. Breast cancer patients that exhibited a higher expression of the target genes of the lncRNAs had a higher metastasis-free survival rate. Conclusion: The current study is the first to identify lncRNAs that are regulated by the presence of Rg3 and KRG extract and that subsequently contribute to inhibiting the proliferation of cancer cells.

• International Journal of Internet, Broadcasting and Communication
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• v.11 no.2
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• pp.67-75
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• 2019

"No IP, No Content" has become a phenomenon in the content industry, high-quality IP has a strategic importance. It has become a Trinity in the movie-anime-game basic package, Competition is more intense. However, there is a tremendous amount of know-how hidden behind the use of IP to operate games well. We are worth exploring in detail. The research and analysis of digital IP market, the advantages and disadvantages will be the focus of our pragmatic research. As an emerging market in the digital industry, China has great research value. This paper analyzes the status quo of the current Chinese market by comparing the mature US and Japanese markets. For example, the research of American Disney Company analyzes the mature market structure of Japan. compared with the excellent case of the Chinese market legend of qin. By studying the current situation of China's digital market, analyzing the interest trends of the customer base, discovering existing problems and improving the accuracy of the prediction and judgment of the Chinese digital market in the future.According to the survey, the IP heat is mainly concentrated in six categories of games, animation, TV, variety, movies, and novels. At present, the most popular IP of manufacturers have three major categories. This article will conduct research and analysis on digital IP, and analyze the market status of China, the United States, and Japan and the research on outstanding representative works in the market.

• The Journal of the Convergence on Culture Technology
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• v.9 no.4
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• pp.503-508
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• 2023

Tryptane derivatives are substances that treat acute migraines, and many studies have been conducted on analysis methods such as chromatography, electrochemistry, spectroscopy, and capillary electrophysiology. Recently, analytical chemists have become more interested in drug analysis and solving fundamental problems of biological importance. Therefore, in this study, the chemical properties of each derivative were investigated by calculating the total energy, band gap, electrostatic potential, and charge of Sumatriptan, Lizatriptan, Naratriptan, and Eletriptan using HyperChem8.0's semi-empirical PM3 method. As a result of this study, in the case of Sumatriptan, Naratriptan, and Eletriptan, chemical reactions are expected to proceed centering on oxygen and nitrogen atoms bonded to sulfur atoms. In addition, in the case of Rizatriptan without a sulfur atom, it was shown that the chemical reaction proceeds at the 17th and 19th nitrogens of the 5-membered heterocyclic compound.

• Steel and Composite Structures
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• v.50 no.2
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• pp.201-216
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• 2024

This paper is motivated by the lack of studies relating to vibration and nonlinear resonance of fluid-conveying cantilever porous GPLR pipes with fractional viscoelastic model resting on nonlinear foundations. A dynamical model of cantilever porous Graphene Platelet Reinforced (GPLR) pipes conveying fluid and resting on nonlinear foundation is proposed, and the vibration, natural frequencies and primary resonant of such system are explored. The pipe body is considered to be composed of GPLR viscoelastic polymeric pipe with porosity in which Halpin-Tsai scheme in conjunction with fractional viscoelastic model is used to govern the construction relation of the nanocomposite pipe. Three different porosity distributions through the pipe thickness are introduced. The harmonic concentrated force is also applied on pipe and excitation frequency is close to the first natural frequency. The governing equation for transverse motion of the pipe is derived by the Hamilton principle and then discretized by the Galerkin procedure. In order to obtain the frequency-response equation, the differential equation is solved with the assumption of small displacement, damping coefficient, and excitation amplitude by the multiple scale method. A parametric sensitivity analysis is carried out to reveal the influence of different parameters, such as nanocomposite pipe properties, fluid velocity and nonlinear viscoelastic foundation coefficients, on the primary resonance and linear natural frequency. Results indicate that the GPLs weight fraction porosity coefficient, fractional derivative order and the retardation time have substantial influences on the dynamic response of the system.