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Monosaccharide as a Central Scaffold Toward the Construction of Salicylate-Based Bidentate PTP1B Inhibitors via Click Chemistry

  • Tang, Yan-Hui;Hu, Min;He, Xiao-Peng;Fahnbulleh, Sando;Li, Cui;Gao, Li-Xin;Sheng, Li;Tang, Yun;Li, Jia;Chen, Guo-Rong
    • Bulletin of the Korean Chemical Society
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    • v.32 no.3
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    • pp.1000-1006
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    • 2011
  • The discovery of carbohydrate-based bioactive compounds has recently received considerable interest in the drug development. This paper stresses on the application of 1-methoxy-O-glucoside as the central scaffold, whereas salicylic pharmacophores were introduced with diverse spatial orientations probing into the structural preference of an enzymatic target, i.e. protein tyrosine phosphatase 1B (PTP1B). By employing regioselective protection and deprotection strategy, 2,6-, 3,4-, 4,6- and 2,3-di-O-propynyl 1-methoxy-O-glucosides were previously synthesized and then coupled with azido salicylate via click chemistry in forming the desired bidentate salicylic glucosides with high yields. The inhibitory assay of the obtained triazolyl derivatives leads to the identification of the 2,3-disubstituted salicylic 1-methoxy-O-glucoside as the structurally privileged PTP1B inhibitor among this bidentate compound series with micromole-ranged $IC_{50}$ value and reasonable selectivity over other homologous PTPs tested. In addition, docking simulation was conducted to propose a plausible binding mode of this authorized inhibitor with PTP1B. This research might furnish new insight toward the construction of structurally different bioactive compounds based on the monosaccharide scaffold.

Measurement System of Dynamic Liquid Motion using a Laser Doppler Vibrometer and Galvanometer Scanner (액체거동의 비접촉 다점측정을 위한 레이저진동계와 갈바노미터스캐너 계측시스템)

  • Kim, Junhee;Shin, Yoon-Soo;Min, Kyung-Won
    • Journal of the Computational Structural Engineering Institute of Korea
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    • v.31 no.5
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    • pp.227-234
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    • 2018
  • Researches regarding measurement and control of the dynamic behavior of liquid such as sloshing have been actively on undertaken in various engineering fields. Liquid vibration is being measured in the study of tuned liquid dampers(TLDs), which attenuates wind motion of buildings even in building structures. To overcome the limitations of existing wave height measurement sensors, a method of measuring liquid vibration in a TLD using a laser Doppler vibrometer(LDV) and galvanometer scanner is proposed in this paper: the principle of measuring speed and displacement is discussed; a system of multi-point measurement with a single point of LDV according to the operating principles of the galvanometer scanner is established. 4-point liquid vibration on the TLD is measured, and the time domain data of each point is compared with the conventional video sensing data. It was confirmed that the waveform is transformed into the traveling wave and the standing wave. In addition, the data with measurement delay are cross-correlated to perform singular value decomposition. The natural frequencies and mode shapes are compared using theoretical and video sensing results.

A Study on the Casual Wear Design based on the Image of the Modernized Korean Costume (생활한복 이미지를 활용한 캐주얼웨어 디자인 개발)

  • Park Young-Seon
    • Journal of the Korean Society of Costume
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    • v.55 no.1 s.91
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    • pp.25-42
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    • 2005
  • Costume is a formative art expressed by active human unlike the field of other living formativeness, and an expression of social actions based on a style of culture in a period. Therefore, costume has a deep connection with a mode of living and is recognized as a 'culture for living', and is more characteristic culture than all metaphysical cultures including architecture, craft, painting, and sculpture. Therefore, it expresses wearer's status or social standing, and furthermore, ideas and values of the times with aesthetic features in their form, color, materials, and pattern, so it is expressed as a mirror reflecting the phases of the times as. Korean costume had been dressed until the period of the Joseon Dynasty without a great change and started to be simplified in a simple style on the grounds of inconvenience in behaviors with the opening of an interchange of Western culture in the civilized period. And, this movement had been continued and Korean costume had been applied as an everyday dress under the name of 'Reformed Korean Costume'. Since the middle phase of 1980s, it aroused many people's interests with the introduction of designs focused on activity and convenience. In 1990's, many people had taken a growing interest in Korean costume with development of various designs keeping pace with the internationalization period and Korean Costume had been revitalized under the name of 'The Modernized Korean Costume'. And, since the 21st century, the advanced communication and full-scaled import of Western fashion have made the introduction of many fashion information in the world into Korea, affected greatly the fashion market, led consumers' sensitivity on a trend to be increased. Therefore, a design accepting a trend 'The Modernized Korean Costume' with fashions has risen. Second, this study is an attempt to suggest a revitalization method of domestic casual Korean costume brands by developing and suggesting competitive and highly value-added products with connection of practicality, variety, and highly sensitive fashion styles. For theoretical study, domestic and foreign literatures, academic journals, professional monthly magazines, and newspapers were examined. And, a process of change and features of the Korean fashion since the civilization period, and concept, features and images of casual Korean costume were analyzed, On the basis of analyzing image, features, and consumers' preference of the modernized Korean costume, a design development plan was established and 10 suits of costume were designed and made.

CORRELATION BETWEEN VASCULAR ENDOTHELIAL GROWTH FACTOR EXPRESSION AND MALIGNANCY GRADING IN BIOPSY SPECIMENS OF TONGUE CANCERS (설암의 술전 조직표본에서 악성도와 혈관내피세포성장인자 발현과의 상관관계)

  • Byun, June-Ho;Park, Bong-Wook;Chung, In-Kyo;Kim, Jong-Ryoul;Kim, Uk-Kyu;Park, Bong-Soo;Kim, Gyoo-Cheon
    • Maxillofacial Plastic and Reconstructive Surgery
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    • v.27 no.6
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    • pp.528-534
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    • 2005
  • Angiogenesis is important for the growth and metastasis of solid tumors. Some growth factors, inflammatory cytokines, and angiogenin are known to promote tumor angiogenesis. Among them, Vascular endothelial growth factor (VEGF) is the most intriguing factor in regard to tumor angiogenesis. Inhibition of VEGF activity by neutralizing antibodies or by the introduction of dominant negative VEGF receptors into endothelial cells of tumor-associated blood vessels resulted in the inhibition of tumor growth and in tumor regression, indicating that VEGF is a major initiator of tumor angiogenesis. VEGF promotes angiogenesis through their receptors, Flt-1 and Flk-1/KDR. on vascular endothelial cells. These two receptors were usually believed to be expressed specifically on vascular endothelial cell. Several reports have now shown that VEGF is not only significantly associated with microvessel density but also has prognostic value in both node-negative and node-positive oral squamous cell carcinoma. For many years several histologic features of the neoplasms are being considered when assessing the influence of malignancy grading on recurrence and prognosis. Among the characteristics investigated, degree of keratinization, nuclear pleomorphism, mode of invasion, microscopic depth of invasion, intravascular invasion, lymphocyte infiltration, and number of mitoses have been considered as important prognostic factors. So, this study was conducted to evaluate the correlation of vascular endothelial growth factor expression with malignancy in paraffin-embedded biopsy specimens from 11 patients with tongue cancers. Our results showed that high immunoreactivity specimens of VEGF expression were significantly lower keratinization degree and more pronounced nuclear pleomorphism than in low immunoreactivity specimens. Thus, VEGF expression could be used as a prognostic marker in tongue cancer.

Development of ultrafine grained silicon carbide by spark plasma sintering (스파크 플라즈마 소결에 의한 초미세 결정립 탄화규소의 개발)

  • 조경식;이광순;백성호;이상진
    • Journal of the Korean Crystal Growth and Crystal Technology
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    • v.13 no.4
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    • pp.176-181
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    • 2003
  • Rapid densification of a SiC powder with additive 0.5 wt% $B_4$C was conducted by spark plasma sintering (SPS). The unique features of the process are the possibilities of using very fast heating rate and short holding time to obtain fully dense materials. The heating rate and applied pressure were kept to be $100^{\circ}C$/min and 40 MPa, while sintering temperature and soaking time varied to 1800, 1850, 1900 and $1950^{\circ}C$ and 10, 20 and 30 min, respectively. All of the SPS-sintered specimens at $1950^{\circ}C$ reached near-theoretical density. The XRD found that 3C-to-6H transformation at $1850^{\circ}C$. The microstructures of the rapidly densified SiC ceramics consisted of duplex microstructure with ultrafine equiaxed grains under 2 $\mu\textrm{m}$ and elongated grains of 0.5∼2 $\mu\textrm{m}$ wide, length 3∼10 $\mu\textrm{m}$. The biaxial strength increased with the increase of sintering time. Strength of 392.7 MPa was obtained with the fully densified specimen sintered at $1950^{\circ}C$ for 30 min, in agreement with the general tendency that strength increases with decreases pore. On the other hand, the fracture toughness shows the value of 2.17∼2.34 MPa$.$$m^{1/2}$ which might be due to the transgranular fracture mode.

Comparison of an Analytic Solution of Wind-driven Current and all (x-$\sigma$) Numerical Model (취송류의 해석위와 (x-$\sigma$) 수치모형과의 비교)

  • 이종찬;최병호
    • Journal of Korean Society of Coastal and Ocean Engineers
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    • v.4 no.4
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    • pp.208-218
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    • 1992
  • Analytic solutions for the gradient of surface elevation and vertical profiles of velocity driven by the wind stress in the one-dimensional rectangular basin were obtained under the assumption of steady-state. The approach treats the bottom frictional stress $\tau$$_{b}$ as known and includes vertically varying eddy viscosity $textsc{k}$$_{M}$, which is constant, linear and quadratic of water depth. When the $\tau$$_{b}$ is param-terized with surface stress, depth averaged velocity and bottom velocity, the result shows the relation of the no-slip bottom velocity condition and the bottom frictional stress $\tau$$_{b}$. The results of a mode splitted, (x-$\sigma$) coordinate, numerical model were compared with the derived analytic solutions. The comparison was made for the case such that $textsc{k}$$_{M}$ is the constant, linear and quadratic function of water depth. In the case of constant $textsc{k}$$_{M}$, the gradient of surface elevation and vertical profiles of velocity are discussed for a uniform depth, a mild slope and a relatively steep slope. When $textsc{k}$$_{M}$ is a linear and quadratic function of water depth, the vertical structures of velocities are discussed for various $\tau$$_{b}$. The result of the comparison shows that the vertical structure of velocities depends not only on the value of $textsc{k}$$_{M}$ but also on the profile of $textsc{k}$$_{M}$ and bottom stress $\tau$$_{b}$. Model results were in a good agreement with the analytic solutions considered in this study.his study.y.his study.

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A Study on Biological Activities of Fermented Jujube and Grape (대추 및 포도 발효물의 생리활성 효과에 관한 연구)

  • Park, Tae-Soon;Kim, Dong-Hee;Kwon, O-Jun;Son, Jun-Ho
    • Microbiology and Biotechnology Letters
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    • v.42 no.2
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    • pp.106-113
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    • 2014
  • For the development of high value consumables utilizing jujube and grape, we investigated the biological activities of a variety of existing fermentation products of jujube and grape. The results revealed that ethanol fermentation products of jujube and grape had a higher antioxidative activity than acetic acid fermentation products. In addition, the ethanol fermentation products of jujube (JEF) had the highest antioxidative activity, with it being greater than that of the ethanol fermentation products of grape (GEF), the acetic acid fermentation products of jujube (JAF) and the acetic acid fermentation products of grape (GAF). As regards tests on whitening effects, JEF exhibited the highest tyrosinase inhibition effects amongst the test groups. However, when immunofluorecence was employed, JAF was seen to inhibit the expression of proteins related to the whitening effect. In the lipopolysaccharide-stimulated mode peritoneal macrophage model, all tested groups of fermentation products (JEF, GEF, JAF and GAF) suppressed nitric oxide production dose-dependently, with ethanol fermentation products demonstrating a higher nitric oxide expression inhibition effect than acetic acid fermentation products. When subjected to antibacterial activity tests, GAF exhibited antibacterial activity against all tested strains except Propionibacterium acnes. Both GAF and JEF revealed high antibacterial activity against Escherichia coli.

Effects of Vertical Eddy Viscosity on the Velocity Profile - Cases of Given Vertical Eddy viscosity - (鉛直 過粘性係數가 流速의 鉛直構造에 미치는 影響 - 鉛直 過粘性係數가 주어진 境遇 -)

  • 이종찬;최병호
    • 한국해양학회지
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    • v.29 no.2
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    • pp.119-131
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    • 1994
  • Vertical structures of wind-driven and tidal currents in a rectangular shaped uniform-depth basin of homogeneous water have been investigated using a mode-splitted, multi-level grid-box, hydrodynamic numerical model. The model was verified using analytical solutions for various vertical eddy viscosity profiles such as: a constant eddy viscosity, a linearly decreasing or increasing variation with depth, a quadratic variation with depth and an exponential variation with depth. Particular attention has been paid on the effects of "near-surface wall layer" on vertical shear of velocity. In numerical calculations, the whole water depth was divided into 13 levels with an unequal grid spacing. the model satisfactorily reproduces the velocity profile, but in case the eddy viscosity decreases rapidly with depth as in quadratical or exponential variation with depth, the vertical gradient of velocity near the bottom became very steep, and analytical solutions and numerical results showed some discrepancy. The vertical structures of horizontal velocity vary with both the depth-averaged value of eddy viscosity and its profiles. the velocity near the sea surface and near the bottom responded sensitively to the eddy viscosity of wall layer. For wind-driven current, the strong velocity shear was generated near the sea surface as eddy viscosity near the surface became small. For tidal current, the velocity above the sea bottom layer was almost constant regardless of the profiles of vertical eddy viscosity, but velocity in the sea bottom layer showed strong shear as eddy viscosity became small.

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The Typhoon Surge in the Southern Coast of Korea (한국 남해안의 태풍에 의한 해일)

  • Jang, Seon-Deok;Lee, In-Cheol;Park, Cheol-Seok
    • Journal of the Korean Society of Fisheries and Ocean Technology
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    • v.27 no.4
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    • pp.293-302
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    • 1991
  • The anomalous sea level deviation or storm surge caused by the typhoon Thelma in 1987 are studied analysing tidal observation data at 7 stations in the south coast of Korean peninsula. The surges are calculated by subtracting the predicted tidal height from the observed tidal record. The tidal deviation at these stations along the coast are discussed in association with meteorological data. The sea level anomalies are studied by means of the empirical orthogonal function (EOF) analysis and the fast fourier transform (FFT) method. The results of analysis suggest that the peak value of surges are higher at the tidal stations in semi-enclosed bay and in long narrow channel than at the ones facing with the open sea. From the result of EOF analysis, the temporal and spatial fluctuations of storm surge can be described by the first EOF mode, which explains 63% of the total variances during the passage of typhoon Thelma. The deviation of storm surge in the studied areas indicates bi-modal peak during the passage of typhoon Thelma. From the results of FFT spectrum analysis, the peak of energy of autospectrum for surge, atmospheric pressure, and wind stress appeared at low frequency fluctuations band of 0.008-0.076 cph over the 4 stations. Auto-correlation function of surge showed periodicity, while that of atmospheric pressure and wind stress indicates no periodicity. The result of FFT analysis shows that the typhoon surges are related chiefly with the change of atmospheric pressure in an open bay (Cheju Harbor), but with the wind stress in a semi-enclosed bay (Yeosu Harbor).

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Effects of Exclusive Agency Listing and Real Estate Information Network System on Real Estate Broker' Trust and Customer' Satisfactions (전속중개계약과 부동산거래정보망제도가 중개업자 신뢰성과 고객만족에 미치는 영향 분석)

  • Choi, Bong-hyun;Moon, Young-kee
    • Journal of Distribution Science
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    • v.4 no.2
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    • pp.123-144
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    • 2006
  • For the property right's protection of the nation, the uncertainty's dissolution and the reliability's security of real estate trade are very important. With the life style's change, the market of real estate becomes diversification, and the level of the real estate trade becomes diversification. But compared with this, the trade system of the real estate has not broken away from the mode in the past yet. To cope with it actively, it needs to review the real estate trade form. Especially, it needs to investigate a plan that can advance the Agency Listing method. The Exclusive Agency Listing and the real estate Information Network System have been the usual system in some advanced countries like America, Japan. It is the system that establishes the real estate brokerage's trade order and encourages the execution for the real estate client's property right's protection and benefit offer. In our country, The Exclusive Agency Listing and the real estate Information Network System were created in the revised real estate brokerage law in 12, 1993. But because of varies of questions, it can not be settled down. So this paper will develop the characteristic factors of the Exclusive Agency Listing and the real estate Information Network System revitalization and examine the mutual relation depends on the factors. And these factors were studied through the proved analysis to the effecting made on the Agency function's consideration and real estate broker' trust and customer satisfaction. So depends on these, the existed value now will present the revitalization plan and political implication about the Exclusive Agency Listing and the real estate Information Network System.

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