• Title/Summary/Keyword: e-Ring

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Synthesis and HIV-1 Integrase Inhibitory Activities of 4-Hydroxy-5-azacoumarin 3-Carboxamides

  • Lee, Seung-Uk;Park, Jang-Hyun;Kwon, Tae-Hoon;Yoo, Yeong-Jae;Lee, Jae-Yeol;Shin, Cha-Gyun;Yoo, Kyung-Ho;Lee, Yong-Sup
    • Bulletin of the Korean Chemical Society
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    • v.28 no.9
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    • pp.1510-1514
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    • 2007
  • Recently, it has been reported that the inhibition of the strand transfer function of HIV-1 integrase is necessary to obtain significant antiviral activity. Accordingly, several compounds typified by aryl 1,3-diketo acids that can inhibit strand transfer reaction of HIV-1 IN have been identified. In this work, we synthesized new 4- hydroxy-5-azacoumarin-3-carbox(thio)amides (1a-h) and evaluated for the inhibition of HIV-1 IN strand transfer reaction with a brief SAR. Among synthesized, compound 1e was the most potent HIV-1 IN inhibitor with equipotent activity to that of L-708,906. Therefore, the 4-hydroxy-5-azacoumarin ring can be considered as a new scaffold in designing more potent of HIV-1 IN inhibitors for treatment of AIDS.

Aminolysis of 2,4-Dinitrophenyl 2-Furoate and 2-Thiophenecarboxylate: Effect of Modification of Nonleaving Group from Furoyl to Thiophenecarbonyl on Reactivity and Mechanism

  • Um, Ik-Hwan;Min, Se-Won;Chuna, Sun-Mee
    • Bulletin of the Korean Chemical Society
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    • v.29 no.7
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    • pp.1359-1363
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    • 2008
  • Second-order rate constants have been determined spectrophotometrically for reactions of 2,4-dinitrophenyl 2- thiophenecarboxylate (2) with a series of alicyclic secondary amines in 80 mol % $H_2O$/20 mol % DMSO at 25.0 ${\pm}$ 0.1 ${^{\circ}C}$. The Brønsted-type plot exhibits a downward curvature, i.e., the slope decreases from 0.74 to 0.34 as the amine basicity increases. The $pK_a$ at the center of the Brønsted curvature, defined as $pK_a^o$, has been determined to be 9.1. Comparison of the Brønsted-type plot for the reactions of 2 with that for the corresponding reactions of 2,4-dinitrophenyl 2-furoate (1) suggests that reactions of 1 and 2 proceed through a common mechanism, although 2 is less reactive than 1. The curved Brønsted-type plot has been interpreted as a change in RDS of a stepwise mechanism. The replacement of the O atom in the furoyl ring by an S atom (1 $\rightarrow$ 2) does not alter the reaction mechanism but causes a decrease in reactivity. Dissection of the apparent second-order rate constants into the microscopic rate constants has revealed that the $k_2/k_{-1}$ ratio is not influenced upon changing the nonleaving group from furoyl to thiophenecarbonyl. However, $k_1$ has been calculated to be smaller for the reactions of 2 than for the corresponding reactions of 1, indicating that the C=O bond in the thiophenecarboxylate 2 is less electrophilic than that in the furoate 1. The smaller k1 for the reactions of 2 is fully responsible for the fact that 2 is less reactive than 1.

Opposing Effects of Arkadia and Smurf on TGFβ1-induced IgA Isotype Expression

  • Choi, Seo-Hyun;Seo, Goo-Young;Nam, Eun-Hee;Jeon, Seong-Hyun;Kim, Hyun-A;Park, Jae-Bong;Kim, Pyeung-Hyeun
    • Molecules and Cells
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    • v.24 no.2
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    • pp.283-287
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    • 2007
  • $TGF-{\beta}1$ induces Ig germ-line ${\alpha}$ ($GL{\alpha}$) transcription and subsequent class switching recombination (CSR) to IgA. In the present study, we investigated the roles of two E3-ubiquitin ligases, Smurfs (HECT type) and Arkadia (RING finger type) on $TGF{\beta}1$-induced IgA CSR. We found that over-expression of Smurf1 and Smurf2 decreased $TGF{\beta}1$-induced $GL{\alpha}$ promoter activity and strengthened the inhibitory effect of Smad7 on the promoter activity. Further, over-expression of Smurf1 and Smurf2 decreased both Smad3/4-mediated and Runx3-mediated $GL{\alpha}$ promoter activities, suggesting that the Smurfs can down-regulate the major $TGF-{\beta}1$ signaling pathway and decrease $GL{\alpha}$ gene expression. In parallel, the over-expressed Smurf1 decreased the expression of endogenous IgA CSR-predictive transcripts ($GLT_{\alpha}$, $PST_{\alpha}$, and $CT_{\alpha}$) and also $TGF{\beta}1$-induced IgA secretion. Conversely over-expression of Arkadia abolished the inhibitory effect of Smad7 on $TGF{\beta}1$-induced $GLT_{\alpha}$ expression and IgA secretion. Similar results were obtained in the presence of over-expressed Smad7 and Smurf1. These results indicate that Arkadia can amplify $TGF{\beta}1$-induced IgA CSR by degrading Smad7, which interacts with Smurf1. We conclude that Smurf and Arkadia have opposite roles in the regulation of $TGF{\beta}1$-induced IgA isotype expression.

Research of Grip Forces and Subjective Preferences for Various Individual Finger Grip Spans by using an (MFFM System을 이용한 손가락 별 파지 폭들의 변화에 따른 악력 및 개인 선호도에 대한 연구)

  • Kim, Dae-Min;Kong, Yong-Ku
    • Journal of the Ergonomics Society of Korea
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    • v.27 no.3
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    • pp.1-6
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    • 2008
  • Individual finger/total grip forces, and subjective preferences for various individual finger grip spans (i.e., four fingers had identical grip spans or different grip spans) were evaluated by using an "Adjustable Multi-Finger Force Measurement (MFFM) System". In this study, three grip spans were defined as follows: a 'favorite grip span' which is the span with the highest subjective preference; a 'maximum grip span' which is the span with the highest total grip force; a 'maximum finger grip span' which is a set of four grip spans that had maximum finger grip forces associated with the index, middle, ring, and little fingers, respectively. Ten males were recruited from university population for this study. In experiment I, each participant tested the maximum grip force with five grip spans (45 to 65mm) to investigate grip forces and subjective preferences for three types of grip spans. Results showed that subjective preferences for grip spans were not coincidence with the performance of total grip forces. It was noted that the 'favorite grip span' represented the lowest total grip force, whereas the 'maximum finger grip span' showed the lowest subjective preferences. The individual finger forces and the average percentage contribution to the total finger force were also investigated in this study. The findings of this study might be valuable information for designing ergonomics hand-tools to reduce finger/hand stress as well as to improve tool users' preferences and performance.

Changes in the Species of Woods Used for Korean Ancient and Historic Architectures (우리나라 건축물에 사용된 목재 수종의 변천)

  • Park, Won-Kyu;Lee, Kwang-Hee
    • Journal of architectural history
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    • v.16 no.1
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    • pp.9-28
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    • 2007
  • We investigated the changes in the species of the woods used for Korean ancient and historic architectures, which include prehistoric excavated relics and existing wooden buildings in South Korea. The species data were collected from various sources such as excavation and repair reports, journal papers, and a few unpublished documents. We divided the building Periods as Paleolithic, Neolitic, Bronze Ages, Iron Age/Three Kingdoms, Koryo, Joseon (early, middle, late) and modem periods. In prehistoric periods, hardwoods were major species. Oak (Quercus spp.) woods dominated (94 percent in average); the others (5%) were Juglans mandshurica, Platycarya strobilacea, Castanea crenata, and few softwoods(1%). During Iron Age and Three Kingdom periods, oaks remained as a major species (57%) and others Platycarya strobilacea(21%), Castanea crenata(13%), and Pinus spp. (6%). The oak woods decreased in Koryo period and they occupied only 1.1%. Instead of oaks, pine (Pinus spp., 71%) and Zelkova serrata (22%) dominated in Koryo. In early and middle Joseon periods, pine woods (73%) remain as a major species and the others were oaks (14%) and Zelkova serrata (9%). As late Joseon came, the pine woods occupied more than 88%. In the late 19th and early 20th centuries, a few boreal species such as larch (Larix spp.) and spruce (Picea spp.), which grow in cold area, were found. We believe they were transported from northern Korea. The existing buildings in Korea are mainly from Joseon period and a few from late Koryo periods. During these periods, pine woods were used for most buildings. For such reason, pine woods were known as 'representative materials for historic buildings'. but earlier times, broad-leaved trees, i.e., oak and Zelkova woods were major materials. The changes in building materials resulted from both climate and human impacts. The dry climate and disturbed forests induce more pines in the mountains. We also compared the wood qualities of the species and found that Zelkova woods were superior ones and deserved more planting for future demands in the repair for historic buildings.

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Preparation and Pore-Characteristics Control of Nano-Porous Materials using Organometallic Building Blocks

  • Oh, Gyu-Hwan;Park, Chong-Rae
    • Carbon letters
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    • v.4 no.1
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    • pp.1-9
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    • 2003
  • Recently, the control of pore-characteristics of nano-porous materials has been studied extensively because of their unique applications, which includes size-selective separation, gas adsorption/storage, heterogeneous catalysis, etc. The most widely adopted techniques for controlling pore characteristics include the utilization of pillar effect by metal oxide and of templates such as zeolites. More recently, coordination polymers constructed by transition metal ions and bridging organic ligands have afforded new types of nano-porous materials, porous metal-organic framework(porous MOF), with high degree and uniformity of porosity. The pore characteristics of these porous MOFs can be designed by controlling the coordination number and geometry of selected metal, e.g transition metal and rare-earth metal, and the size, rigidity, and coordination site of ligand. The synthesis of porous MOF by the assembly of metal ions with di-, tri-, and poly-topic N-bound organic linkers such as 4,4'-bipyridine(BPY) or multidentate linkers such as carboxylates, which allow for the formation of more rigid frameworks due to their ability to aggregate metal ions into M-O-C cluster, have been reported. Other porous MOF from co-ligand system or the ligand with both C-O and C-N type linkage can afford to control the shape and size of pores. Furthermore, for the rigidity and thermal stability of porous MOF, ring-type ligand such as porphyrin derivatives and ligands with ability of secondary bonding such as hydrogen and ionic bonding have been studied.

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DETECTION OF WIDE PLANETARY SYSTEM WITH MICROLENSING

  • Ryu, Yoon-Hyun;Park, Myeong-Gu;Chang, Heon-Young;Lee, Ki-Won
    • The Bulletin of The Korean Astronomical Society
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    • v.37 no.2
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    • pp.108.2-108.2
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    • 2012
  • Recent results from microlensing surveys show that a free-floating planet or a wide-separation planet is more numerous than a main-sequence star in the Galaxy. Moreover, the detection efficiency of the planets will be improved in next-generation experiments with a high survey monitoring frequency. However, microlensing events produced by both planets appear similar light curves with a short duration timescale, thus it is difficult to distinguish them. In this paper, we investigated the detectable separation range of a wide-separation planet as the planet bound to its host star. We construct the fractional deviation maps using the magnifications of the planetary lensing and the single-lensing by planet itself for various parameters such as a mass ratio, separation, and source radius. As a result, we found that the pattern of the fractional deviation is related to the ratio of source radius to caustic size, and the ratio satisfying the detection criterion (i.e., ${\geq}5%$ in the fractional deviation) varies with a separation. Hence, we derived a fitting formula as the function of a mass ratio and a source radius to reflect the variation in the calculations of the detectable separation range of a wide-separation planet as the planet bound to its host star. In addition, we estimated the condition that a wide-separation planet can be detected as a single-lensing event under the finite source effect. We found that such a case is possible provided that the source radius is smaller than ~2.5 times of Einstein ring radius of a planet, regardless of a separation or a mass ratio.

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Electroplating process for the chip component external electrode

  • Lee, Jun-Ho
    • Proceedings of the Korean Institute of Surface Engineering Conference
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    • 2000.11a
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    • pp.1-2
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    • 2000
  • In chip plating, several parameters must be taken into consideration. Current density, solution concentration, pH, solution temperature, components volume, chip and media ratio, barrel geometrical shape were most likely found to have an effect to the process yields. The 3 types of barrels utilized in chip plating industry are the onventional rotating barrel, vibrational barrel(vibarrel), and the centrifugal type. Conventional rotating barrel is a close type and is commonly used. The components inside the barrel are circulated by the barrel's rotation at a horizontal axis. Process yield has known to have higher thickness deviation. The vibrational barrel is an open type which offers a wide exposure to electrolyte resulting to a stable thickness deviation. It rotates in a vertical axis coupled with multi-vibration action to facilitate mixed up and easy transportation of components. The centrifugal barrel has its plated work centrifugally compacted against the cathode ring for superior electrical contact with simultaneous rotary motion. This experiment has determined the effect of barrel vibration intensity to the plating thickness distribution. The procedures carried out in the experiment involved the overall plating process., cleaning, rinse, Nickel plating, Tin-Lead plating. Plating time was adjusted to meet the required specification. All other parameters were maintained constant. Two trials were performed to confirm the consistency of the result. The thickness data of the experiment conducted showed thatbthe average mean value obtained from higher vibrational intensity is nearer to the standard mean. The distribution curve shown has a narrower specification limits and it has a reduced variation around the target value. Generally, intensity control in vi-barrel facilitates mixed up and easy transportation of components. However, it is desirable to maintain an optimum vibration intensity to prevent solution intrusion into the chips' internal electrode. A cathodic reaction can occur in the interface of the external and internal electrode. 2H20 + e $\rightarrow$M/TEX> 20H + H2.. Hydrogen can penetrate into the body and create pressure which can cause cracks. At high intensity, the chip's motion becomes stronger, its contact between each other is delayed and so plating action is being controlled. However, the strong impact created by its collision can damage the external electrode's structure there by resulting to bad plating condition.

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Distribution of Nematophagous Fungi Under Different Habitats (서식 환경에 따른 선충잡이곰팡이의 종류와 분포)

  • Kim, Dong-Geun;Bae, Su-Gon;Shin, Yong-Seub
    • The Korean Journal of Mycology
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    • v.29 no.2
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    • pp.123-126
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    • 2001
  • A survey of 43 soil samples collected from southern Korea has shown that nematophagous fungi occurred in a variety of habitats. Nine predatory and two endoparasitic species were isolated. Habitats were classified into four types, i. e., mountain, upland, paddy field and greenhouse. Of these, greenhouse and upland had the highest incidence of nematophagous fungi $(95{\sim}100%)$ compared with mountain (37.5%) and paddy field (16.7%). The most common species was Arthrobotrys oligospora Fres., which was isolated from 25.5% of soil samples. Net forming species were the most abundant (72.5%), followed by constricting ring (10.0%), adhesive hyphae (7.8%), endoparasitic fungi (5.0%), and adhesive knob (4.8%). Nematophagous fungi were isolated move frequently from cultivated soil rather than uncultivated mountainous soil.

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Cloning and Expression Characteristics of Pharbitis nil COP1 (PnCOP1) During the Floral Induction

  • Kim, Yun-Hee;Kim, Seong-Ryong;Heo, Yoon-Kang
    • Journal of Photoscience
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    • v.12 no.1
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    • pp.1-9
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    • 2005
  • The ubiquitin E3 ligase COP1 (Constitutive Photomorphogenesis 1) is a protein repressor of photomorphogenesis in Arabidopsisplants, and it found in various organisms, including animals. The COP1 protein regulates the stability of many of the light-signaling components that are involved in photomorphogenesis and in the developmental processes. To study the effect of COP1 on flowering in a short day plant, we have cloned a full-length of PnCOP1 (Pharbitis nil COP1) cDNA from Pharbitis nil Choisy cv. Violet, and we examined its transcript levels under various conditions. A full-length PnCOP1 cDNA consists of 2,280 bp nucleotidesthat contain 47 bp of 5'-UTR, 232 bp of 3'-UTR including the poly (A) tail, and 1,998 bp of the coding sequence. The deduced amino acid sequence contains 666 amino acids, giving it a theoretical molecular weight of 75 kD and a isolectric point of 6.2. The PnCOP1 contains three distinct domains, an N-terminal $Zn^2+$-binding RING-finger domain, a coiled-coil structure, and WD40 repeats at the C-terminal, implying that the protein plays a role in protein-protein interactions. The PnCOP1 transcript was detected in the cotyledon, hypocotyls and leaves, but not in root. The levels of the PnCOP1 transcript were reduced in leaves that were a farther distance away from the cotyledons. The expression level of the PnCOP1 gene was inhibited by light, while the expression was increased in the dark. During the floral inductive 16 hour-dark period for Pharbitis nil, the expression was increased and it reached its maximum at the 12th hour of the dark period. The levels of PnCOP1 mRNA were dramatically reduced upon light illumination. These results suggest that PnCOP1 may play an important function in the floral induction of Pharbitis nil.

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