• Bulletin of the Korean Chemical Society
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• 제35권12호
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• pp.3590-3594
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• 2014

Blue phosphorescent $(dfpypy)_2Ir(mppy)$, where dfpypy = 2',6'-difluoro-2,3'-bipyridine and mppy = 5-methyl-2-phenylpyridine, has been synthesized by newly developed effective method and its solid state structure and photoluminescent properties are investigated. The glass-transition and decomposition temperature of the compound appear at $160^{\circ}C$ and $360^{\circ}C$, respectively. In a crystal packing structure, there are two kinds of intermolecular interactions such as hydrogen bonding ($C-H{\cdots}F$) and edge-to-face $C-H{\cdots}{\pi}(py)$ interaction. This compound emits bright blue phosphorescence with ${\lambda}_{max}=472nm$ and quantum efficiencies of 0.23 and 0.32 in fluid and the solid state. The emission band of the compound is red-shifted by 40 nm relative to homoleptic congener, $Ir(dfpypy)_3$. The ancillary ligand in $(dfpypy)_2Ir(mppy)$ has been found to significantly destabilize HOMO energy, compared to $Ir(dfpypy)_3$, $(dfpypy)_2Ir(acac)$ and $(dfpypy)_2Ir(dpm)$, without significantly changing LUMO energy.

• Genomics & Informatics
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• 제6권1호
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• pp.36-43
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• 2008

Radiotherapy would be the choice of treatment for human cancers, because of high cost-effectiveness. However, a certain population of patients shows a resistance to radiotherapy and recurrence. In an effort to increase the efficacy of radiotherapy, many efforts were driven to find the genes causing the unresponsiveness to ionizing radiation. In this paper, we compared the gene expression profiles of two lung cancer cell lines, H460 and H1299, which showed differential responses to ionizing radiations. Each cell were irradiated at 2 Gy, and harvested after 0, 2, 4, 8, 12 and 24 hours to examine the expressions. Two-way ANOVA analysis on time-series experiments of two cells could select 2863 genes differentially expressed upon ionizing radiation among 32,321 genes in microarray (p<0.05). We classified these genes into 21 clusters by SOM clustering according to the interaction between cell types and time. Two SOM clusters were enriched with apoptosis-related genes in pathway analysis. One cluster contained higher levels of phosphatidyl inositol 3-phosphate kinase (PI3K) subunits in H1299, radio-resistant cells than H460, radiosensitive cells. TRAIL receptors were expressed in H460 cells while the decoy receptor for TRAIL was expressed in H1299 cells. From these results, we could characterize the differential responsiveness to ionizing radiation according to their differential expressions of apoptosis-related genes, which might be the candidates to increase the power of radiotherapy.

• 대한바이러스학회지
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• 제27권1호
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• pp.69-75
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• 1997

To evaluate in vitro anti-HIV efficacies of nucleoside derivatives, MT-4 cell line was infected with HIV-1 and HIV-2 respectively and treated with various compounds and the formerly approved drugs such as AZT, d4T, ddC and ddI. CPE method was used to evaluate their antiviral activity. Most dideoxynucleosides, AZT, d4T, ddC and ddI, showed anti-HIV activities against both viruses but no other compounds including anti-herpesvirus drugs did any. Further experiments were carried out to study their inhibitory mechanism of viral adsorption. The results showed no inhibition of syncytium formation due to an interaction between the gp120 expressed in HIV -infected cell surface and CD4 receptor on the uninfected cell surface in the presence of AZT. AZT showed no activity up to $100\;{\mu}g/ml$. Inhibition of reverse transcriptase (RT) in the presence of AZT-triphosphate was tested by using RT expressed in E. coli and purified and its $IC_{50}$ was 4.5 nM.

• Molecules and Cells
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• 제44권1호
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• pp.50-62
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• 2021

Among all cancer types, lung cancer ranks highest worldwide in terms of both incidence and mortality. The crosstalk between lung cancer cells and their tumor microenvironment (TME) has begun to emerge as the "Achilles heel" of the disease and thus constitutes an attractive target for anticancer therapy. We previously revealed that crosstalk between lung cancer cells and endothelial cells (ECs) induces chemoresistance in multicellular tumor spheroids (MCTSs). In this study, we demonstrated that factors secreted in response to crosstalk between ECs and lung cancer cells play pivotal roles in the development of chemoresistance in lung cancer spheroids. We subsequently determined that the expression of hypoxia up-regulated protein 1 (HYOU1) in lung cancer spheroids was increased by factors secreted in response to crosstalk between ECs and lung cancer cells. Direct interaction between lung cancer cells and ECs also caused an elevation in the expression of HYOU1 in MCTSs. Inhibition of HYOU1 expression not only suppressed stemness and malignancy, but also facilitated apoptosis and chemosensitivity in lung cancer MCTSs. Inhibition of HYOU1 expression also significantly increased the expression of interferon signaling components in lung cancer cells. Moreover, the activation of the PI3K/AKT/mTOR pathway was involved in the HYOU1-induced aggression of lung cancer cells. Taken together, our results identify HYOU1, which is induced in response to crosstalk between ECs and lung cancer cells within the TME, as a potential therapeutic target for combating the aggressive behavior of cancer cells.

• Steel and Composite Structures
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• 제34권1호
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• pp.1-15
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• 2020

This paper presents experimental and numerical studies on effects of local damages on the in-plane elastic-plastic buckling and strength of a fixed parabolic steel tubular arch under a vertical load distributed uniformly over its span, which have not been reported in the literature hitherto. The in-plane structural behaviour and strength of ten specimens with different local damages are investigated experimentally. A finite element (FE) model for damaged steel tubular arches is established and is validated by the test results. The FE model is then used to conduct parametric studies on effects of the damage location, depth and length on the strength of steel arches. The experimental results and FE parametric studies show that effects of damages at the arch end on the strength of the arch are more significant than those of damages at other locations of the arch, and that effects of the damage depth on the strength of arches are most significant among those of the damage length. It is also found that the failure modes of a damaged steel tubular arch are much related to its initial geometric imperfections. The experimental results and extensive FE results show that when the effective cross-section considering local damages is used in calculating the modified slenderness of arches, the column bucking curve b in GB50017 or Eurocode3 can be used for assessing the remaining in-plane strength of locally damaged parabolic steel tubular arches under uniform compression. Furthermore, a useful interaction equation for assessing the remaining in-plane strength of damaged steel tubular arches that are subjected to the combined bending and axial compression is also proposed based on the validated FE models. It is shown that the proposed interaction equation can provide lower bound assessments for the remaining strength of damaged arches under in-plane general loading.

• 한국환경농학회지
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• 제39권1호
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• pp.36-43
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• 2020

본 연구는 낙동강수계 중권역 중 최대의 농업용수 관개면적을 가지는 위천수계를 대상으로 관개용수에 대한 기초자료 마련을 위해 수리화학적 특성과 관개용 수질특성을 평가하였다. 위천수계의 유기물 오염도와 염분 함량을 나타내는 평균 BOD₅ 농도와 EC는 각각 1.1 mg/L, 350 µS/cm로 좋은 수질을 보였고, 이 중 남천은 BOD₅ 0.5 mg/L, EC 157 µS/cm로 가장 낮아 매우 깨끗한 수질을 나타내었다. 위천은 각 지류와 하수처리방류수가 유입되는 쌍계천의 합류로 인해 하류로 갈수록 염분 농도가 미미하게 증가하였으나 영향은 크지 않았다. 금속류에 대해서도 매우 안전한 수질을 보여 토양과 농산물 재배에 미치는 유해성은 없는 것으로 나타났다. 위천수계의 미네랄 형성은 탄산염암 풍화로 인한 물-암석 교환작용의 영향이 우세한 것으로 나타났고, Ca-HCO₃-Cl 수질유형에 집중분포 하였다. 위천수계의 양이온과 음이온에 대한 분포농도는 각각 Ca²⁺>Mg²⁺>Na⁺>K⁺, HCO₃^->SO₄^2->Cl^-> F^- 순으로 존재하였다. 이들 성분에 대해 남천은 다른 하천에 비해 2배 이상 낮은 농도분포를 보였다. 구천의 경우 Ca²⁺과 SO₄^2-농도는 다른 하천보다 각각 1.2-3.2배, 1.6-3.1배 높게 형성하고 있었다. SAR, %Na, PI, RSC 지수를 평가한 결과 위천수계 수질은 염분의 영향이 매우 낮아 농산물 재배에 적합한 관개용수로 나타났다. 특히 염분농도는 벼 수확량에 미치는 영향이 크므로 위천수계의 대표 농작물인 벼 재배를 위한 매우 중요한 수질인자이다. 위천수계는 FAO와 국내 연구자료에서 제시한 벼 재배에 대한 염분 허용농도기준을 충분히 만족하였고, 다른 농작물 생산에도 전혀 피해가 없는 우수한 수질을 갖는 것으로 나타났다. 앞으로 본 연구결과가 농산물 재배 및 우수성 홍보 등에 기초자료로 활용되어 지역 농업활동에 도움이 되길 기대한다.

• 생명과학회지
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• 제30권9호
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• pp.826-833
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• 2020

Phospholipase C gamma (PLCγ)는 phosphatidylinositol을 가수분해하여 신호전달 과정에 참여하는 PLC의 주요한 isotype으로 γ-specific array의 특징적인 구조를 바탕으로 receptor tyrosine kinases 및 non-receptor tyrosine kinase 신호를 주로 매개한다. PLCγ1과 PLCγ2의 두 isozyme이 존재하며 다양한 세포에서 발현하여 cell proliferation, migration 및 differentiation 등 여러 세포작용을 조절하고 있다. 최근의 연구들에서 PLCγ 돌연변이가 cancer와 immune disease 및 brain disorder 등에 연관된다는 것이 밝혀지고 있으며 genetic model을 통해 PLCγ의 생리적·병리적 기능이 제시되었다. 본 리뷰에서는 최신의 연구 결과들을 바탕으로 PLCγ의 구조와 활성 조절 기전에 대해 기술하고 나아가 여러 질병의 발병과 진행에서 보고된 PLCγ의 돌연변이와 knockout 마우스를 활용한 연구 결과를 바탕으로 생리적·병리적 관점에서 PLCγ의 역할에 대해 고찰하였다.

• Archives of Pharmacal Research
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• 제28권9호
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• pp.1002-1012
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• 2005

5-Substituted 4-oxo-2-thioxo-1,,2,3,4-tetrahydropyrimidine were synthesized by interaction of 4­oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonylhydrazide with some aldehydes to give the corresponding Schiff-bases, which after cyclization gave corresponding thiazolidinones. For some of the thiazolidinones, Mannich bases reaction was carried out. All the derivatives were tested for their possible inhibitory effect on Schistosoma mansoni cercarial elastase (CE). Only, N'-(4-methylbenzyledine)-4-oxo-2-thioxo-1,2 ,3,4-tetrahydropyrimidine-5-sulfonylhydrazide was found to have potent inhibitory effect on the CE activity with $IC_{50} = 264{\mu}M.$ Upon its use as a paint for mice tails before infection with S. mansoni cercariae, the compound formulated in jojoba oil caused a significant reduction ($93\%$; P-value = 0.0002) in the worm burden. IgG & IgM in mice sera were measured by using several S. mansoni antigens by ELISA. Sera from treated infected mice (TIM) 2, 4, and 6 weeks (W) post infection (PI) showed 1.2 folds lower, 1.2 folds higher, 1.7 folds lower IgM reactivity against soluble cercarial antigenic preparation (CAP), respectively, when compared with sera collected from infected untreated mice (IUM). Sera from TIM 2, 4, and 6WPI showed 1.3, 1.6, and 1.7 folds higher IgG reactivity, respectively against CAP than the IgG reactivity from IUM. Sera from TIM 2, 4 and 6WPI showed 1.5, 1.2 folds lower and 1.4 folds higher IgM reactivity, respectively against soluble worm antigenic preparation (SWAP) when compared with sera collected from IUM. Sera from TIM 2, 4, and 6WPI showed 1.4, 1 folds lower and 1 fold higher IgG reactivity, respectivley to SWAP when compared with sera from IUM. Sera from TIM 2, 4, and 6WPI had generaly lower IgM and IgG reactivities against soluble egg antigen (SEA) when compared with sera from IUM.

• Biomolecules & Therapeutics
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• 제20권1호
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• pp.27-35
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• 2012

Oroxylin A is a flavone isolated from a medicinal herb reported to be effective in reducing the inflammatory and oxidative stresses. It also modulates the production of brain derived neurotrophic factor (BDNF) in cortical neurons by the transactivation of cAMP response element-binding protein (CREB). As a neurotrophin, BDNF plays roles in neuronal development, differentiation, synaptogenesis, and neural protection from the harmful stimuli. Adenosine $A2_A$ receptor colocalized with BDNF in brain and the functional interaction between $A2_A$ receptor stimulation and BDNF action has been suggested. In this study, we investigated the possibility that oroxylin A modulates BDNF production in cortical neuron through the regulation of $A2_A$ receptor system. As expected, CGS21680 ($A2_A$ receptor agonist) induced BDNF expression and release, however, an antagonist, ZM241385, prevented oroxylin A-induced increase in BDNF production. Oroxylin A activated the PI3K-Akt-GSK-$3{\beta}$ signaling pathway, which is inhibited by ZM241385 and the blockade of the signaling pathway abolished the increase in BDNF production. The physiological roles of oroxylin A-induced BDNF production were demonstrated by the increased neurite extension as well as synapse formation from neurons. Overall, oroxylin A might regulate BDNF production in cortical neuron through $A2_A$ receptor stimulation, which promotes cellular survival, synapse formation and neurite extension.

• 한국환경성돌연변이발암원학회지
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• 제26권4호
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• pp.125-132
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• 2006

Previous studies showed that epigallocatechin gallate(EGCG) have substantial effects of suppressing the N-methyl-N'-nitro-N-nitrosoguanidine(MNNG)-initiated cell transformation process on the bases of foci formation frequency and loss of anchorage dependency. In this study we tried to clarify the molecular mechanism of suppressing the cell transformation process. Mouse cell line balb/c 3T3 A31-1-1 was exposed 2 days to MNNG followed by 15 days 12-O-tetradecanoylphorbol-13-acetate(TPA) treatment for our transformation process. EGCG was added after the time point of 24 hours exposure to TPA and incubated for 19 days. 2029 genes were selected in our transformation process that showed fold change value of 1.5 or more in the microarray gene expression analysis covering the mouse full genome. These genes were found to be involved mainly in the cell cycle pathway, focal adhesion, adherens junction, TGE-$\beta$ signaling, apoptosis, lysine degradation, insulin signaling, ECM-receptor interaction. Among the genes, we focused on the 631 genes(FC>0.5) reciprocally affected by EGCG treatment. Our study suggest that EGCG down-regulate the gene expressions of up stream signaling factors such as nemo like kinase with MAPK activity and PI3-Kinase, Ras GTPase and down stream factors such as cyclin D1, D2, H, T2, cdk6.