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Effect of Double Replacement of L-Pro, D-Pro, D-Leu or Nleu in Hydrophobic Face of Amphipathic α-Helical Model Antimicrobial Peptide on Structure, Cell Selectivity and Mechanism of Action

  • Shin, Song Yub
    • Bulletin of the Korean Chemical Society
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    • v.35 no.11
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    • pp.3267-3274
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    • 2014
  • In order to investigate the effects of the double replacement of $\small{L}$-Pro, $\small{D}$-Pro, $\small{D}$-Leu or Nleu (the peptoid residue for Leu) in the hydrophobic face (positions 9 and 13) of amphipathic ${\alpha}$-helical non-cell-selective antimicrobial peptide $L_8K_9W_1$ on the structure, cell selectivity and mechanism of action, we synthesized a series of $L_8K_9W_1$ analogs with double replacement of $\small{L}$-Pro, $\small{D}$-Pro, $\small{D}$-Leu or Nleu in the hydrophobic face of $L_8K_9W_1$. In this study, we have confirmed that the double replacement of $\small{L}$-Pro, $\small{D}$-Pro, or Nleu in the hydrophobic face of $L_8K_9W_1$ let to a great increase in the selectivity toward bacterial cells and a complete destruction of ${\alpha}$-helical structure. Interestingly, $L_8K_9W_1$-$\small{L}$-Pro, $L_8K_9W_1$-$\small{D}$-Pro and $L_8K_9W_1$-Nleu preferentially interacted with negatively charged phospholipids, but unlike $L_8K_9W_1$ and $L_8K_9W_1$-$\small{D}$-Leu, they did not disrupt the integrity of lipid bilayers and depolarize the bacterial cytoplasmic membrane. These results suggested that the mode of action of $L_8K_9W_1$-$\small{L}$-Pro, $L_8K_9W_1$-$\small{D}$-Pro and $L_8K_9W_1$-Nleu involves the intracellular target other than the bacterial membrane. In particular, $L_8K_9W_1$-$\small{L}$-Pro, $L_8K_9W_1$-$\small{D}$-Pro and $L_8K_9W_1$-Nleu had powerful antimicrobial activity (MIC range, 1 to $4{\mu}M$) against methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant Pseudomonas aeruginosa (MDRPA). Taken together, our results suggested that $L_8K_9W_1$-$\small{L}$-Pro, $L_8K_9W_1$-$\small{D}$-Pro and $L_8K_9W_1$-Nleu with great cell selectivity may be promising candidates for novel therapeutic agents, complementing conventional antibiotic therapies to combat pathogenic microorganisms.

Dicumarol Inhibits PMA-Induced MMP-9 Expression through NQO1-independent manner in Human Renal Carcinoma Caki Cells (인간 신장암 Caki세포에서 dicumarol에 의한 PMA 매개 matrix metalloproteinase-9의 발현 억제 효과)

  • Park, Eun Jung;Kwon, Taeg Kyu
    • Journal of Life Science
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    • v.26 no.2
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    • pp.174-180
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    • 2016
  • Dicumarol is a coumarin derivative isolated from sweet clover (Melilotus alba), and has anti-coagulant activity with the inhibitory activity of NAD(P)H quinone oxidoreductase1 (NQO1). NQO1 catalyzes the two-electron reduction of quinones to hydroquinones. Dicumarol competes with NAD(P)H for binding to NQO1, resulting in the inhibition of NQO1 enzymatic activity. The expression of matrix metalloproteinases (MMPs) has been implicated in the invasion and metastasis of cancer cells. The expression of MMPs is regulated by cytokines and signal transduction pathways, including those activated by phorbol myristate acetate (PMA). However, the effects of dicumarol on metalloproteinase (MMP)-9 expression and activity are not investigated here. This study investigated whether dicumarol inhibits MMP-9 expression and activity in PMA-treated human renal carcinoma Caki cells. Dicumarol markedly inhibited the PMA-induced MMP-9 mRNA expression and MMP-9 activity. NF-κB and AP1 promoter activity, which is important in MMP-9 expression, also decreased in dicumarol-treated cells. Furthermore, dicumarol markedly suppressed the ability of PMA-mediated migration in Caki cells. When the relevance of NQO1 in the dicumarol-mediated inhibitory effect on PMA-induced MMP9 activity was elucidated, knock-down of NQO1 with siRNA was found to have no effect on PMA-induced MMP9 activity, suggesting that the stimulating effect of dicumarol on PMA-induced MMP9 activity is independent of NQO1 activity. Taken together, the present studies suggested that dicumarol may inhibit PMA-induced migration via down-regulation of MMP-9 expression and activity.

QTL Analysis of Germination Rate and Germination Coefficient of Velocity under Low Temperature in Rice (저온에서 벼의 발아율 및 발아속도 관련 양적형질 유전자좌(QTL) 분석)

  • Kim, Jinhee;Mo, Youngjun;Ha, Su-Kyung;Jeung, Ji-Ung;Jeong, Jong-Min
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.66 no.1
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    • pp.8-17
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    • 2021
  • As rice originates from tropical regions, low temperature stress during the germination stage in temperate regions leads to serious problems inhibiting germination and seedling establishment. Identifying and characterizing quantitative trait loci (QTLs) for low-temperature germination (LTG) resistance help accelerate the development of rice cultivars with LTG tolerance. In this study, we identified QTLs for LTG tolerance (qLTG5, qLTG9) and germination coefficient of velocity under optimal conditions (OGCV) (qOGCV7, qOGCV9) using 129 recombinant inbred lines (RILs) derived from the cross between a low-temperature sensitive line Milyang23 and a low-temperature tolerant variety Gihobyeo. qLTG9 and qOGCV9 were detected at the same location on chromosome 9. At both LTG QTLs (qLTG5 and qLTG9), the alleles for LTG tolerance were contributed by the japonica variety Gihobyeo. At qOGCV7 and qOGCV9, the alleles for low temperature tolerance were derived from Milyang23 and Gihobyeo, respectively. The RILs with desirable alleles at two or more QTLs, i.e., GroupVII: qLTG5+qLTG9 (qOGCV9) and GroupVIII: qLTG5+qOGCV7+qLTG9 (qOGCV9), showed stable tolerance under low-temperature stress. Our results are expected to contribute to the improvement of tolerance to low-temperature and anaerobic stress in japonica rice, which would lead to the wide adoption of direct-seeding practices.

Seasonal Occurrence of Euzophera batangensis and Attractiveness of Its Sex Pheromone Gland Components in Non-astringent Persimmon Orchards (단감 과수원에서 밤알락명나방의 발생소장과 성페로몬샘 성분의 유인력)

  • Kim, Junheon;Roh, Gwang Hyun;Jang, Sin Ae;Park, Chung Gyoo
    • Korean journal of applied entomology
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    • v.56 no.2
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    • pp.165-169
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    • 2017
  • Seasonal occurrence of persimmon bark borer moth, Euzophera batangensis, and attractiveness of its sex pheromone gland components and trap types were studied at sweet (non-astringent) persimmon orchards of two southern provinces of Gyeongsangnam-do and Jeollanam-do, Korea, from 2014 to 2016. E. batangensis occurred three times a year. Occurrences of the moths of the over-wintered, the $1^{st}$ and the $2^{nd}$ generations were early April to late May, early June to late July, and early August to mid October, respectively. The (Z9,E12)-tetradeca-9,12-dien-1-ol (Z9,E12-14OH) was more attractive than (Z)-tetradec-9-en-1-ol (Z9-14OH). The Z9,E12-14OH was equally attractive to the 9:1 binary mixture of Z9,E12-14OH and Z9-14OH to the male moths. The three trap types of funnel, white and red delta traps had no effect on the attractiveness of the components.

Synthesis of C9-Alcohol through C9-Aldehyde Hydrogenation over Copper Catalysts (구리 촉매 상에서 C9-알데히드의 수소화 반응에 의한 C9-알코올 합성)

  • Park, Young-Kwon;Noh, Sang Gyun;Cho, Kyu Sang;Jeon, Jong-Ki
    • Korean Chemical Engineering Research
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    • v.44 no.4
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    • pp.363-368
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    • 2006
  • This study selected the optimal catalyst for the process of producing $C_9$-alcohol by hydrogenating $C_9$-aldehyde, and carried out an experiment in order to establish the operating condition for maximizing the yield of $C_9$-alcohol. The BET surface area and the specific area of copper were most excellent in $CuO/ZnO/Al_2O_3$ (60:30:10 wt%) catalyst produced using acetate as a precursor of copper and $Na_2CO_3$ as a precipitant, and the catalyst also showed the highest performance in $C_9$-aldehyde hydrogenation. Using a trickle bed reactor loaded with optimized catalyst, we attained 94.1 wt% yield of $C_9$-alcohol under the condition of $175^{\circ}C$, 800 psi and $WHSV=3hr^{-1}$. According to the result of comparing with other catalysts used in the hydrogenation of aldehyde, the catalyst showed similar performance to that of Ni/kieselghur and higher than that of $Cu-Ni-Cr-Na/Al_2O_3$ and $Ni-Mo/Al_2O_3$. According to the result of examining the stability of the catalyst through a long-term catalysis test, the yield of $C_9$-alcohol decreased slowly after around 72 hours due to the increasing production of high boiling-point byproducts.

Design of Unified Inverse Transformer for HEVC and VP9 (HEVC 및 VP9 겸용 통합 역변환기의 설계)

  • Jung, Seulkee;Lee, Seongsoo
    • Journal of IKEEE
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    • v.19 no.4
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    • pp.596-602
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    • 2015
  • In this paper, a unified inverse transformer is designed for HEVC and VP9. The proposed architecture performs all modes of HEVC and VP9 in the unified inverser transformer, such as $4{\times}4{\sim}32{\times}32$ HEVC IDCT, $4{\times}4$ HEVC IDST, $4{\times}4{\sim}32{\times}32$ VP9 IDCT, $4{\times}4{\sim}16{\times}16$ VP9 IADST and $4{\times}4$ IWHT. Same computations are used in HEVC IDCT and VP9 IDCT, except for the scales of the coefficients. Similarly, same computations are used in HEVC $4{\times}4$ IDST and VP9 $4{\times}4$ IADST, except for the scales of the coefficients. Furthermore, HEVC IDCT, VP9 IDCT, and VP9 IADST are the subsets of upper level IDCTs. The proposed architecture reuses multipliers when the computation is identical. Also it shares adders and butterfly structures even when the multiplier coefficients are different. So it reduces the hardware size significantly. Synthesized in 0.18 um technology, the gate count is 456,442 gates. which achieved 22.6% reduction compared to conventional architectures.

과기총9주년의 발자취-과학기술인의 핵심체로 급성장

  • Korean Federation of Science and Technology Societies
    • The Science & Technology
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    • v.8 no.9 s.76
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    • pp.8-10
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    • 1975
  • 한국과학기술계를 총망라한 과기총은 9월24일로 창립 9주년을 맞이하게 되었다. 과학기술인의 핵심체로 급성장한 과기총은 그동안 무섯을 어떻게 했나 지난 9주년동안의 업적을 여기에 간추려 보기로 한다.

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서독 과학기술개발 투자근황

  • Korean Federation of Science and Technology Societies
    • The Science & Technology
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    • v.10 no.2 s.93
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    • pp.9-9
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    • 1977
  • 서독의 1976년도 연구개발 투자 총액은 2백 42억 마르크(4조9,126억만원)이었다. 이것은 서독 GNP의 약 2.2%에 해당되는 거금이다. 서독연구기술부(성) 발표에 의하면 1962년도 서독의 연구개발비가 44억9천 마르크 (9.114억7천만원)로서 서독 GNP의 약 1.1%였었다.

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