• Title/Summary/Keyword: effective models

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Antitumor Activity of LB42907, a Potent and Selective Farnesyltransferase Inhibitor: Synergistic Effect in Combination with Other Anticancer Drugs

  • Park, Ji-Hyun;Koo, Sun-Young;Kim, Dong-Myung;Kim, Kwi-Hwa;Jeong, Shin-Wu;Chung, Hyun-Ho;Cho, Heung-Soo;Park, Joong-Hoon;Yim, Hyeon-Joo;Lee, Jin-Ho;Koh, Jong-Sung;Kim, Se-Mi
    • Bulletin of the Korean Chemical Society
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    • v.29 no.7
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    • pp.1303-1310
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    • 2008
  • Inhibitors of farnesyltransferase (FT), a key enzyme in the post-translational modifications of Ras proteins, have been extensively studied as novel anticancer agents in the preclinical stages, some of which are currently in clinical development. Previously, it has been reported that a novel FT inhibitor LB42907 inhibits Ras farnesylation in the nanomolar range in vitro. The aim of this study was to assess the antitumor efficacy of LB42907 in vitro and in vivo. Anchorage-independent growth of various human tumor cell lines was potently inhibited by treatment with LB42907, comparable to other FT inhibitors in clinical development. In the nude mouse, oral administration of LB42907 demonstrated potent antitumor activity in several human tumor xenograft models including bladder, lung and pancreas origin. Interestingly, significant tumor regression in EJ (bladder) and A549 (lung) xenografts was induced by LB42907 treatment. The effectiveness of LB42907 was also investigated in simultaneous combination with paclitaxel, vincristine, cisplatin or gemcitabine against NCI-H460, A549, and HCT116 cells in vitro using median-effect analysis. LB42907 markedly synergized with most anticancer drugs tested in this study in NCI-H460 cell. In contrast, LB42907 displayed antagonism or partial synergism with these drugs in A549 and HCT116 cells, depending on the class of combined drugs and/ or the level of cytotoxicity. Our results demonstrate that LB42907 is an effective antitumor agent in vitro and in vivo and combination of LB42907 with other chemotherapeutic drugs results in synergistic or antagonistic effects mainly in a cell line-dependent manner. Further preclinical study is warranted.

Drying Characteristics of Osmotically Pre-treated Carrots (삼투처리한 당근의 건조 특성)

  • Youn, Kwang-Sup;Choi, Yong-Hee
    • Korean Journal of Food Science and Technology
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    • v.28 no.6
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    • pp.1126-1134
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    • 1996
  • The physical characteristics changes of carrots during drying were studied to minimize the quality degradation by applying improved drying process and pretreatment method. Physico-chemical properties of the product were analyzed, and then, drying mechanisms were explained by diffusion coefficients and drying models. In hot air drying process, the drying and rehydration efficiencies were high at low relative humidity and high temperature. Browning degree and specific volume also showed similar trend to drying efficiency. Diffusion coefficient, which describes moisture transfer, was also high at low relative humidity and at high temperature. It was verified using. Arrhenius equation that drying process was influenced by temperature. It was also observed during experiment that temperature changes were more effective in drying than relative humidity changes. Quadratic model was the most fittable in explaining the process. As a result of analyzing the experimental data with respect to the drying time, the contents of carotene and moisture could be modeled as a polynomial. As the air velocity increased, drying performance and rehydration efficiency increased.

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3D Digital Design Optimization Process Considering Constructability of Freeform Structure (비정형 구조물의 시공성을 고려한 3차원 디지털 설계 최적화 프로세스)

  • Ryu, Han-Guk
    • Korean Journal of Construction Engineering and Management
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    • v.14 no.5
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    • pp.35-43
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    • 2013
  • Nowadays the widely used media in architecture include visualizations, animations and three-dimensional models. 3D digital methods using active CAM(Computer Aided Manufacturing) and CNC(Computerized Numerical Control) imaging have been developed for accurate shape and 3D measurements in freeform buildings. In contrast to a conventional building using auto CAD system and others, the proposed digital optimization method is based on a combination of 3D numerical data and parametric 3D model for design and construction. The objective of this paper is therefore to present digital optimization process for constructability of freeform building. The method can be useful in the effective implementation of an error-proofing process of freeform building during design and construction phase. 3D digital coordinate data can be used effectively to identify correct size of structural and finish members and installation location of each members in construction field. In addition, architects, engineers and contractors can evaluate design, materials, constructability and identify error-proofing opportunities. Other project participants can also include representatives from all levels of management, departments as well as workers and key subcontractors' personnel, if necessary. The 3D digital optimization process is therefore appropriate to serious variations in freeform shape. For future study, the developed digital optimization method is necessary to be carried out to verify the robustness and accuracy for constructability in construction field.

A Study on the Feasibility of Geomagnetic Declination Investigation at Unified Control Points in South Korea (국내 통합기준점에서 지자기 편각 조사의 타당성 연구)

  • Lee, Yong Chang
    • Journal of Korean Society for Geospatial Information Science
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    • v.24 no.3
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    • pp.29-38
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    • 2016
  • As publicizing of electromagnetic devices such as smart_phone and drone etc. which are relate with geomagnetic direction, and recognition about the importance to space weather effect and their hazards rises up recently, it is required heavily that the study on the effective measurement of geomagnetic declination and geomagnetic field effects of space weather. The purpose of this study is that the investigation of the feasibility of the absolute geomagnetic measurement in a place, where man-made geomagnetic contamination is low or negligible, with replacing the azimuth marks used for the absolute geomagnetic declination measurement with unified control points(UCP) which established at suburb. Further to this, have first derived the correlation of daily variations and disturbance level between the published indices($K_P$ and $K_K$) and geomagnetic element calculated from geomagnetic data of Cheongyang observatory located at the middle stage in Korea and is a member of INTERMAGNET. In addition, have carried out that the absolute measurement for the geomagnetic declination at three places near unified control point and one place with wide open field in Korea. The world magnetic models(WMMs) are selected as the criteria for comparison on the feasibility of geomagnetic declination investigation near unified control points. We compared deviations of declination from absolute measurement with that obtained from WMMs, also those from WMMs inter-comparison. The result through examination and analysis show that the feasibility of the absolute geomagnetic declination measurement with replacing the azimuth marks with UCP which established at suburb is possible.

Univariate Analysis of Soil Moisture Time Series for a Hillslope Located in the KoFlux Gwangneung Supersite (광릉수목원 내 산지사면에서의 토양수분 시계열 자료의 단변량 분석)

  • Son, Mi-Na;Kim, Sang-Hyun;Kim, Do-Hoon;Lee, Dong-Ho;Kim, Joon
    • Korean Journal of Agricultural and Forest Meteorology
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    • v.9 no.2
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    • pp.88-99
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    • 2007
  • Soil moisture is one of the essential components in determining surface hydrological processes such as infiltration, surface runoff as well as meteorological, ecological and water quality responses at watershed scale. This paper discusses soil moisture transfer processes measured at hillslope scale in the Gwangneung forest catchment to understand and provide the basis of stochastic structures of soil moisture variation. Measured soil moisture series were modelled based upon the developed univariate model platform. The modeling consists of a series of procedures: pre-treatment of data, model structure investigation, selection of candidate models, parameter estimation and diagnostic checking. The spatial distribution of model is associated with topographic characteristics of the hillslope. The upslope area computed by the multiple flow direction algorithm and the local slope are found to be effective parameters to explain the distribution of the model structure. This study enables us to identify the key factors affecting the soil moisture distribution and to ultimately construct a realistic soil moisture map in a complex landscape such as the Gwangneung Supersite.

Dieckol Attenuates Microglia-mediated Neuronal Cell Death via ERK, Akt and NADPH Oxidase-mediated Pathways

  • Cui, Yanji;Park, Jee-Yun;Wu, Jinji;Lee, Ji Hyung;Yang, Yoon-Sil;Kang, Moon-Seok;Jung, Sung-Cherl;Park, Joo Min;Yoo, Eun-Sook;Kim, Seong-Ho;Ahn Jo, Sangmee;Suk, Kyoungho;Eun, Su-Yong
    • The Korean Journal of Physiology and Pharmacology
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    • v.19 no.3
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    • pp.219-228
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    • 2015
  • Excessive microglial activation and subsequent neuroinflammation lead to synaptic loss and dysfunction as well as neuronal cell death, which are involved in the pathogenesis and progression of several neurodegenerative diseases. Thus, the regulation of microglial activation has been evaluated as effective therapeutic strategies. Although dieckol (DEK), one of the phlorotannins isolated from marine brown alga Ecklonia cava, has been previously reported to inhibit microglial activation, the molecular mechanism is still unclear. Therefore, we investigated here molecular mechanism of DEK via extracellular signal-regulated kinase (ERK), Akt and nicotinamide adenine dinuclelotide phosphate (NADPH) oxidase-mediated pathways. In addition, the neuroprotective mechanism of DEK was investigated in microglia-mediated neurotoxicity models such as neuron-microglia co-culture and microglial conditioned media system. Our results demonstrated that treatment of anti-oxidant DEK potently suppressed phosphorylation of ERK in lipopolysaccharide (LPS, $1{\mu}g/ml$)-stimulated BV-2 microglia. In addition, DEK markedly attenuated Akt phosphorylation and increased expression of $gp91^{phox}$, which is the catalytic component of NADPH oxidase complex responsible for microglial reactive oxygen species (ROS) generation. Finally, DEK significantly attenuated neuronal cell death that is induced by treatment of microglial conditioned media containing neurotoxic secretary molecules. These neuroprotective effects of DEK were also confirmed in a neuron-microglia co-culture system using enhanced green fluorescent protein (EGFP)-transfected B35 neuroblastoma cell line. Taken together, these results suggest that DEK suppresses excessive microglial activation and microglia-mediated neuronal cell death via downregulation of ERK, Akt and NADPH oxidase-mediated pathways.

Biomass Regressions of Pinus densiflora Natural Forests of Four Local Forms in Korea (한국산(韓國産) 4개(個) 지역형(地域型) 소나무천연림(天然林)의 물질(物質) 현존량(現存量) 추정식(推定式)에 관(關)한 연구(硏究))

  • Park, In Hyeop;Kim, Joon Seon
    • Journal of Korean Society of Forest Science
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    • v.78 no.3
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    • pp.323-330
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    • 1989
  • Pinass densiflora natural forests of four local forms in Korea were studies to investigate effective biomass estimation method. Dimension analysis was used and three allometric regression models, such as logWt=A+BlogD, logWt=$A+B1ogD^2H$ and 1ogWt=A+BlogD+ClogH were applied to estimate biomass, The most accurate estimation was made by the regression model of logWt=A+BlogD+ClogH where Wt is dry weight, D is diameter at breast height, and H is tree height. However, dry weights of cones and dead branches were remotely related to tree size factor, such as D and H. In the interest of practical use. generalized allometric regressions for all samples trees of four stands were computed and analysis of covariance was used to compare the allometric regressions among the four stands. Based on the test criteria applied in this study, significant differences were found in terms of error variance and regression intercept, not in terms of regression slope. These trends suggest a generalized biomass regression is not valid for accurate estimation over a range of four local form stands.

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The prediction Models for Clearance Times for the unexpected Incidences According to Traffic Accident Classifications in Highway (고속도로 사고등급별 돌발상황 처리시간 예측모형 및 의사결정나무 개발)

  • Ha, Oh-Keun;Park, Dong-Joo;Won, Jai-Mu;Jung, Chul-Ho
    • The Journal of The Korea Institute of Intelligent Transport Systems
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    • v.9 no.1
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    • pp.101-110
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    • 2010
  • In this study, a prediction model for incident reaction time was developed so that we can cope with the increasing demand for information related to the accident reaction time. For this, the time for dealing with accidents and dependent variables were classified into incident grade, A, B, and C. Then, fifteen independent variables including traffic volume, number of accident-related vehicles and the accidents time zone were utilized. As a result, traffic volume, possibility of including heavy vehicles, and an accident time zone were found as important variables. The results showed that the model has some degree of explanatory power. In addition, when the CHAID Technique was applied, the Answer Tree was constructed based on the variables included in the prediction model for incident reaction time. Using the developed Answer Tree model, accidents firstly were classified into grades A, B, and C. In the secondary classification, they were grouped according to the traffic volume. This study is expected to make a contribution to provide expressway users with quicker and more effective traffic information through the prediction model for incident reaction time and the Answer Tree, when incidents happen on expressway

Applicability Evaluation of Flood Inundation Analysis using Quadtree Grid-based Model (쿼드트리 격자기반 모형의 홍수범람해석 적용성 평가)

  • Lee, Dae Eop;An, Hyun Uk;Lee, Gi Ha;Jung, Kwan Sue
    • Journal of Korea Water Resources Association
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    • v.46 no.6
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    • pp.655-666
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    • 2013
  • Lately, intensity and frequency of natural disasters such as flood are increasing because of abnormal climate. Casualties and property damages due to large-scale floods such as Typhoon Rusa in 2002 and Typhoon Maemi in 2003 rapidly increased, and these show the limits of the existing disaster prevention measures and flood forecasting systems regarding irregular climate changes. In order to efficiently respond to extraordinary flood, it is important to provide effective countermeasures through an inundation model that can accurately simulate flood inundation patterns. However, the existing flood inundation analysis model has problems such as excessive take of analysis time and accuracy of the analyzed results. Therefore, this study conducted a flood inundation analysis by using the Gerris flow solver that uses quadtree grid, targeting the Baeksan Levee in the Nakdong River Basin that collapsed because of a concentrated torrential rainfall in August, 2002. Through comparisons with the FLUMEN model that uses unstructured grid among the existing flood inundation models and the actual flooded areas, it determined the applicability and efficiency of the quadtree grid-based flood inundation model of the Gerris flow solver.

Identification of yearly variation in Hwacheon dam inflow using trend analysis and hydrological sensitivity method (경향성 분석과 수문학적 민감도 기법을 이용한 화천댐 유입량의 연별 변동량 규명)

  • Kim, Sang Ug;Lee, Cheol-Eung
    • Journal of Korea Water Resources Association
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    • v.51 no.5
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    • pp.425-438
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    • 2018
  • Existing studies that analyze the causes and effects of water circulation use mostly rainfall - runoff models, which requires much effort in model development, calibration and verification. In this study, hydrological sensitivity analysis which can separate quantitatively the impacts by natural factors and anthropogenic factor was applied to the Hwacheon dam upper basin from 1967 to 2017. As a result of using various variable change point detection methods, 1999 was detected as a statistically significant change point. Especially, based on the hydrological sensitivity analysis using 5 Budyko based functions, it was estimated that the average inflow reduction amount by Imnam dam construction was $1.890\;billion\;m^3/year$. This results in this study was slightly larger than the those by existing researchers due to increase of rainfall and decrease of Hwacheon dam inflow. In future, it was suggested that effective water management measures were needed to resolve theses problems. Especially, it can be suggested that the monthly or seasonal analysis should be performed and also the prediction of discharge for future climate change should be considered to establish resonable measures.