• Title/Summary/Keyword: R-113

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3D QSAR Studies of Mps1 (TTK) Kinase Inhibitors Based on CoMFA

  • Balasubramanian, Pavithra K.;Balupuri, Anand;Cho, Seung Joo
    • Journal of Integrative Natural Science
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    • v.9 no.2
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    • pp.113-120
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    • 2016
  • Monopolar spindle 1 (Mps1) is an attractive cancer target due to its high expression levels in a wide range of cancer cells. Mps1 is a dual specificity kinase. It plays an essential role in mitosis. The high expression od Mps1 was observed in various grades of breast cancers. In the current study, we have developed a CoMFA model of pyridazine derivatives as Mps1 kinase inhibitors. The developed CoMFA model ($q^2=0.797$; ONC=6; $r^2=0.992$) exhibited a good predictive ability. The model was then validated by Leave out five, progressive sampling and bootstrapping and found to be robust. The analysis of the CoMFA contour maps depicted favorable and unfavorable regions to enhance the activity. Bulky positive substitution at $R^3$ position and Negative substitution in $R^1$ position is favored could increase the activity. In contrast, bulky substitution in $R^1$ position is not favored. Our results can be used in designing a potent Mps1 (TTK) inhibitor.

An experimental study for boiling heat transfer enhancement under electric fields (전기장하에서의 비등 열전달 촉진에 관한 실험적 연구)

  • O, Si-Deok;Gwak, Ho-Yeong
    • Transactions of the Korean Society of Mechanical Engineers B
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    • v.20 no.7
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    • pp.2298-2314
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    • 1996
  • Electric field effect on boiling of refrigerants R11, R113, and FC72 has been investigated experimentally. One purpose of the experimental investigation is to determine the effects of the electrode arrangements on electrohydrodynamic boiling of the above mentioned liquids. The test equipment employed in the experiment consists of a shell and tube heat exchanger with six or six and twelve rows of electrode wires around the tube. It has been found that the applied voltage promotes the boiling heat transfer coefficient except FC72. Boiling heat transfer enhancement obtained is about 230% for R11, 280% for R113. It has also been observed that bubbles detached from the tube aggregate at the place where the electrical gradient force balances with the buoyancy one. These aggregated bubbles force to decrease the boiling heat transfer coefficient as well as to reduce the voltage needed to the dielectric breakdown.

Mannosylerythritol lipids ameliorate ultraviolet A-induced aquaporin-3 downregulation by suppressing c-Jun N-terminal kinase phosphorylation in cultured human keratinocytes

  • Bae, Il-Hong;Lee, Sung Hoon;Oh, Soojung;Choi, Hyeongwon;Marinho, Paulo A.;Yoo, Jae Won;Ko, Jae Young;Lee, Eun-Soo;Lee, Tae Ryong;Lee, Chang Seok;Kim, Dae-Yong
    • The Korean Journal of Physiology and Pharmacology
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    • v.23 no.2
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    • pp.113-120
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    • 2019
  • Mannosylerythritol lipids (MELs) are glycolipids and have several pharmacological efficacies. MELs also show skin-moisturizing efficacy through a yet-unknown underlying mechanism. Aquaporin-3 (AQP3) is a membrane protein that contributes to the water homeostasis of the epidermis, and decreased AQP3 expression following ultraviolet (UV)-irradiation of the skin is associated with reduced skin moisture. No previous study has examined whether the skin-moisturizing effect of MELs might act through the modulation of AQP3 expression. Here, we report for the first time that MELs ameliorate the UVA-induced downregulation of AQP3 in cultured human epidermal keratinocytes (HaCaT keratinocytes). Our results revealed that UVA irradiation decreases AQP3 expression at the protein and messenger RNA (mRNA) levels, but that MEL treatment significantly ameliorated these effects. Our mitogen-activated protein kinase inhibitor analysis revealed that phosphorylation of c-Jun N-terminal kinase (JNK), but not extracellular signal-regulated kinase or p38, mediates UVA-induced AQP3 downregulation, and that MEL treatment significantly suppressed the UVA-induced phosphorylation of JNK. To explore a possible mechanism, we tested whether MELs could regulate the expression of peroxidase proliferator-activated receptor gamma ($PPAR-{\gamma}$), which acts as a potent transcription factor for AQP3 expression. Interestingly, UVA irradiation significantly inhibited the mRNA expression of $PPAR-{\gamma}$ in HaCaT keratinocytes, whereas a JNK inhibitor and MELs significantly rescued this effect. Taken together, these findings suggest that MELs ameliorate UVA-induced AQP3 downregulation in HaCaT keratinocytes by suppressing JNK activation to block the decrease of $PPAR-{\gamma}$. Collectively, our findings suggest that MELs can be used as a potential ingredient that modulates AQP3 expression to improve skin moisturization following UVA irradiation-induced damage.

Outcome Measurement and Degree of Economic Contribution for the National R&D Reports (국가 R&D 보고서 원문의 활용성과 및 경제적 기여도 분석)

  • Kwak, Seung-Jin;Choi, Jae-Hwang;Kim, Jeong-Taek;Park, Yong-Jae;Choi, Kiseok
    • Journal of the Korean Society for Library and Information Science
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    • v.49 no.1
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    • pp.113-128
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    • 2015
  • As the major developed countries of the world have realized the importance of common information and its utilization, they have begun to seek a plan that will facilitate manipulation of common information. Despite development of the National R&D activities and its quantitative increase in Korea, its practical use still remains at a lower level. Therefore, it is worthwhile to analyze practical use and economic contribution in order to achieve higher profits. There are two purposes of this study. The first purpose is to draw a conclusion by analyzing the practical uses of the National R&D Reports, and the second purpose is to evaluate economic contributions by the National R&D Reports. In order to achieve the objectives of this study, literature review, survey, focus group interview, and experts' consultation were conducted as a way to deepen research, simultaneously comprising the quantitative and qualitative methods.

ON SOME p(x)-KIRCHHOFF TYPE EQUATIONS WITH WEIGHTS

  • Chung, Nguyen Thanh
    • Journal of applied mathematics & informatics
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    • v.32 no.1_2
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    • pp.113-128
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    • 2014
  • Consider a class of p(x)-Kirchhoff type equations of the form $$\left\{-M\left({\int}_{\Omega}\;\frac{1}{p(x)}{\mid}{\nabla}u{\mid}^{p(x)}\;dx\right)\;div\;({\mid}{\nabla}u{\mid}^{p(x)-2}{\nabla}u)={\lambda}V(x){\mid}u{\mid}^{q(x)-2}u\;in\;{\Omega},\\u=0\;on\;{\partial}{\Omega},$$ where p(x), $q(x){\in}C({\bar{\Omega}})$ with 1 < $p^-\;:=inf_{\Omega}\;p(x){\leq}p^+\;:=sup_{\Omega}p(x)$ < N, $M:{\mathbb{R}}^+{\rightarrow}{\mathbb{R}}^+$ is a continuous function that may be degenerate at zero, ${\lambda}$ is a positive parameter. Using variational method, we obtain some existence and multiplicity results for such problem in two cases when the weight function V (x) may change sign or not.

THE RELATION BETWEEN MCSHANE INTEGRAL AND MCSHANE DELTA INTEGRAL

  • Park, Jae Myung;Lee, Deok Ho;Yoon, Ju Han;Kim, Young Kuk;Lim, Jong Tae
    • Journal of the Chungcheong Mathematical Society
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    • v.27 no.1
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    • pp.113-121
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    • 2014
  • In this paper, we define an extension $f^*:[a,\;b]{\rightarrow}\mathbb{R}$ of a function $f:[a,\;b]_{\mathbb{T}}{\rightarrow}\mathbb{R}$ for a time scale $\mathbb{T}$ and show that f is McShane delta integrable on $[a,\;b]_{\mathbb{T}}$ if and only if $f^*$ is McShane integrable on [a, b].

A CHARACTERIZATION OF M-HARMONICITY

  • Lee, Jae-Sung
    • Bulletin of the Korean Mathematical Society
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    • v.47 no.1
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    • pp.113-119
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    • 2010
  • If f is M-harmonic and integrable with respect to a weighted radial measure $\upsilon_{\alpha}$ over the unit ball $B_n$ of $\mathbb{C}^n$, then $\int_{B_n}(f\circ\psi)d\upsilon_{\alpha}=f(\psi(0))$ for every $\psi{\in}Aut(B_n)$. Equivalently f is fixed by the weighted Berezin transform; $T_{\alpha}f = f$. In this paper, we show that if a function f defined on $B_n$ satisfies $R(f\circ\phi){\in}L^{\infty}(B_n)$ for every $\phi{\in}Aut(B_n)$ and Sf = rf for some |r|=1, where S is any convex combination of the iterations of $T_{\alpha}$'s, then f is M-harmonic.

A study on laser welding characteristics of 1500MPa grade ultra high strength steel for automotive application (자동차용 1500MPa급 초고강도강의 레이저 용접 특성에 관한 연구)

  • Choi, Jin-Kang;Kim, Cheol-Hee;Rhee, Se-Hun
    • Proceedings of the KWS Conference
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    • 2009.11a
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    • pp.113-113
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    • 2009
  • 세계적으로 환경문제에 대한 관심이 커짐에 따라 연료 효율 향상과 매연을 줄이기 위해 차량 경량화 요구가 증가하는 동시에 안전 규제가 강화되고 있어 높은 강도를 가지는 소재의 적용이 증가하고 있다. 충돌 시 차량 구조를 유지시켜주는 범퍼나 B-필러와 같은 부품에 1500MPa급의 초고강도강이 적용되고 있으며 레이저 용접이 가지는 장점이 많이 알려지면서 그 사용이 증가하는 추세이다. 따라서 레이저 용접에 의한 초고강도강의 용접 특성에 대한 연구가 필요하다. 본 연구에서는 1500MPa급 초고강도강의 레이저 맞대기 용접을 실시하여 단면, 경도 측정, 인장시험을 통해 용접부 특성을 파악하였다. 파이버 레이저와 디스크 레이저를 사용하여 각각의 레이저빔 직경 변화에 따른 입열량 변화에 따라 용접성에 미치는 영향에 대해 알아보았다.

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