• Title/Summary/Keyword: Chemical library

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Potent Inhibition of Human Telomerase by Small Chemical Compounds

  • Kim, Joo-Hee;Kim, Jun-Hyun;Lee, Gun-Eui;Chung, In-Kwon
    • Proceedings of the PSK Conference
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    • 2003.10a
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    • pp.96-96
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    • 2003
  • Telomerase activity is expressed in most types of cancer cells but not in normal somatic cells, suggesting that telomerase may be an important target for cancer chemotherapy. Inhibition of telomerase results in telomere erosion leading to the subsequent growth-arrest of cancer cells followed by senescence or cell death. In this study, we screened a chemical library for inhibition of human telomerase, identifying two groups of inhibitors. (omitted)

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Dual Capillary Column System for the Qualitative Gas Chromatography: 2. Comparison between Splitless and On-Column Injection Modes

  • Kim, Kyoung-Rae;Kim, Jung-Han;Park, Hyoung-Kook;Oh, Chang-Hwan
    • Bulletin of the Korean Chemical Society
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    • v.14 no.2
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    • pp.250-255
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    • 1993
  • A dual capillary column system is described for the simultaneous analysis of a given sample and measurement of retention index (RI) and area ratio (AR) values of each peak on two capillary columns of different polarity, DB-5 & DB-1701 from a single injection. Both capillary columns were connected to either a splitless injector or an on-column injector via a deactivated fused-silica capillary tubing of 1 m length and a 'Y' splitter. Both injection modes allowed to measure RI and AR values with high reproducibility (<0.01% RSD) and high accuracy (<10% RE), respectively with the exception that the trace and high boiling solutes required the on-column mode for the accurate quantification and AR comparison. When the dual capillary column system in on-column injection mode was applied to the blind samples containing organic acids, each acid was positively indentified by the combined computer RI library search-AR comparison.

Rice genes specifically expressed in a rice mutant gained resistance to rice blast.(oral)

  • C. U. Han;Lee, C. H.;K. S. Jang;Park, Y. H.;H. K. Lim;Kim, J.C.;Park, G. J.;J.S. Cha;Park, J. E.
    • Proceedings of the Korean Society of Plant Pathology Conference
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    • 2003.10a
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    • pp.66.2-66
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    • 2003
  • A gain-of-function mutant, SHM-11 obtained through gamma-ray mutagenesis, is resistant to rice blast caused by Magnaporthe grisea while wild type Sanghaehyanghyella is highly susceptible to the same disease. The resistance in the mutant was not race-specific when we tested with four races (KJ-201, KI-1113a, KI-313, KI-409) of M. grisea. To identify genes involved disease resistance in the gain-of-function mutant, genes specifically expressed in the mutant were selected by suppression subtractive hybridization using cDNAS of blast-inoculated mutant and wild type as a tester and a driver, respectively, Random 200 clones from the subtracted library were selected and analyzed by DNA sequencing. The sequenced genes represented three major groups related with disease resistance; genes encoding PR proteins, genes probably for phytoalexin biosynthesis, and genes involved in disease resistance signal transduction. A gene encoding a putative receptor-like protein kinase was identified as highly expressed only in the gain-of-function mutant after blast infection. The role of the putative receptor-like protein kinase gene during blast resistance will be further studied.

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A Study on the Planning of Nationwide Indexing Services for Korea (전국색인지간행협동체제 편성방안에 관한 연구)

  • Choi Sung Jin
    • Journal of the Korean Society for Library and Information Science
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    • v.12
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    • pp.39-86
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    • 1985
  • The main purpose of the present study is to survey the major iudexing bulletins of national nature in Korea, to define such problem areas as lacunae, duplicates and limitation in coverage in the indexing services currently available in Korea, and to make some suggestions for action for improving the existing indexing services in the light of general principles and the tradition and constraints unique to Korea. The major findings and conclusions reached at this study are summarised as follows: (A) A new indexing bulletin of general nature covering the entire field needs to be created in each of the following fields without an established indexing service available for the outcome of research and development activities in Korea. (1) Philosophy (2) Religion (3) Pure sciences (4) Art (5) Language (6) Literature (7) History (B) A new specialised indexing bulletin needs to be created in each of the following fields where indexing services are heavily utilised but no, or only partial, indexing service is available. (1) Social sciences (a) Statistics (b) Sociology (c) Folklore (d) Military science (2) Pure sciences (a) Mathematics (b) Physics (c) Chemistry (d) Astronomy (e) Geology (f) Mineralogy (g) Life sciences (h) Botany (i) Zoology (3) Applied sciences (a) Medicine (b) Agriculture (c) Civil engineering (d) Architectural engineering (e) Mechanical engineering (f) Electrical engineering (g) Chemical engineering (h) Domestic science (C) Publication of the indexing bulletins suggested in A and B above may be ideally carried on by a qualified and dependable learned society established in the respective fields and designated by the Minister of Education, and should be financially supported from the public fund under the provisions of Art. 27 of the Scientific Research Promotion Act of 1979. (D) The coverage and contents of the four indexing bulletins in the field of banking and financing published by the Library of the Bank of Korea are similar and considerably duplicated. It is, therefore, suggested that the four indexing bulletins are combined in one to form a more comprehensive and efficient bibliographical tool in the field and it is further developed into a general guide to the literature produced in the entire field of economics in Korea by gradually expanding its subject coverage. (E) For the similar reasons stated in D, the Index to the Articles on North Korea and the Catalogue of Theses on North Korea, both publisheds by the Ministry of Unification Library, are suggested to make into one. The Index to the Articles of the Selected North Korean Journals and the Index to the Articles of the North Korean Journals in Microfilm Housed in the Ministry of Unification Library, both published by the same Library, are also suggested to be combined in one. (F) The contents of the Catalogue of the Reports Submitted by Government Officials Who Have Travelled Abroad, published by the National Archives are included in the Index to the Information Materials Related to Government Administration, published by the National Archives. The publication of the former is hardly justified. (G) The contents of the Index to Legal Literature published by the Seoul National University Libraries and those of the Law Section of the Index to Scholastic Works published by the National Central Library are nearly identical. One of the two indexes should cease to be published. (H) Though five indexes are being published in the field of political science and four in the field of public administration, their subject coverage is limited. Naturally, these indexes are little usable to many other researchers in the two fields. A comprehensive index covering all the specialised areas in each field needs to be developed on one or all the existing indexes. (I) It is suggested that the Catalogue of the Scholastic Works on Curricula published by the National Central Library expands its subject coverage to become a more usable and effective index to all the researchers in the field of education. (J) The bimonthly Index to Periodical Articles and the specialised index by subject series published by the National Assembly Library, and the Index to Scholastic Works published by the National Central Library are expected to increase their coverage and frequency of publication to be used more effectively and more efficiently by all users in all fields till the indexing bulletins suggested in this study will fully be available in Korea.

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Novel Silica Nanotubes Using a Library of Carbohydrate Gel Assemblies as Templates for Sol-Gel Transcription in Binary Systems

  • Jung, Jong-Hwa;Lee, Shim-Sung;Shinkai, Seiji;Iwaura, Rika;Shimizu, Toshimi
    • Bulletin of the Korean Chemical Society
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    • v.25 no.1
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    • pp.63-68
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    • 2004
  • Sugar-based gelator p-dodecanoyl-aminophenyl- ${\beta}$-D-aldopyranosides (1-3) have been shown to self-assemble in the presence of p-aminophenyl aldopyranosides. The hydrogel 1+4 showed the double-helical structure with 3-25 nm outer diameters, which is quite different from that of 1. The gel 2+5 revealed twisted ribbon structure with 30-50 nm in widths and a few micrometers of length whereas the gel 3+4 revealed the single and the bundled fiber structures. The difference in these gel supramolecular structures has successfully been transcribed into silica structures by sol-gel polymerization of tetraethoxysilane (TEOS), resulting in the doublehelical, the twisted-ribbon, the single and the multiple (lotus-shaped) hollow fiber structures. These results indicate that novel silica structures can be created by transcription of various superstructures formed in binary gels through the hydrogen-bonding interaction, and the amino group of the p-aminophenyl aldopyranosides acts as an efficient driving force to create novel silica nanotubes. Furthermore, electron energy-loss spectroscopy (ELLS) provided strong evidence for the inner hollow structure of the double-helical silica nanotube. This is a novel and successful example that a variety of new silica structures can be created using a library of carbohydrate gel fibers as their templates.

Undecanoic Acid, Lauric Acid, and N-Tridecanoic Acid Inhibit Escherichia coli Persistence and Biofilm Formation

  • Jin, Xing;Zhou, Jiacheng;Richey, Gabriella;Wang, Mengya;Choi Hong, Sung Min;Hong, Seok Hoon
    • Journal of Microbiology and Biotechnology
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    • v.31 no.1
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    • pp.130-136
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    • 2021
  • Persister cell formation and biofilms of pathogens are extensively involved in the development of chronic infectious diseases. Eradicating persister cells is challenging, owing to their tolerance to conventional antibiotics, which cannot kill cells in a metabolically dormant state. A high frequency of persisters in biofilms makes inactivating biofilm cells more difficult, because the biofilm matrix inhibits antibiotic penetration. Fatty acids may be promising candidates as antipersister or antibiofilm agents, because some fatty acids exhibit antimicrobial effects. We previously reported that fatty acid ethyl esters effectively inhibit Escherichia coli persister formation by regulating an antitoxin. In this study, we screened a fatty acid library consisting of 65 different fatty acid molecules for altered persister formation. We found that undecanoic acid, lauric acid, and N-tridecanoic acid inhibited E. coli BW25113 persister cell formation by 25-, 58-, and 44-fold, respectively. Similarly, these fatty acids repressed persisters of enterohemorrhagic E. coli EDL933. These fatty acids were all medium-chain saturated forms. Furthermore, the fatty acids repressed Enterohemorrhagic E. coli (EHEC) biofilm formation (for example, by 8-fold for lauric acid) without having antimicrobial activity. This study demonstrates that medium-chain saturated fatty acids can serve as antipersister and antibiofilm agents that may be applied to treat bacterial infections.

Expression and Characterization of Trehalose Biosynthetic Modules in the Adjacent Locus of the Salbostatin Gene Cluster

  • Choeng, Yong-Hoon;Yang, Ji-Yeon;Delcroix, Gaetan;Kim, Yoon-Jung;Chang, Yong-Keun;Hong, Soon-Kwang
    • Journal of Microbiology and Biotechnology
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    • v.17 no.10
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    • pp.1675-1681
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    • 2007
  • The pseudodisaccharide salbostatin, which consists of valienamine linked to 2-amino-1,5-anhydro-2-deoxyglucitol, is a strong trehalase inhibitor. From our Streptomyces albus ATCC 21838 genomic library, we identified thirty-two ORFs in a 37-kb gene cluster. Twenty-one genes are supposed to be a complete set of modules responsible for the salbostatin biosynthesis. Through sequence analysis of the gene cluster, some of the upstream gene products (SalB, SalC, SalD, SalE, and SalF) revealed functional resemblance with trehalose biosynthetic enzymes. On the basis of this rationale, we isolated the five genes (salB, salC, salD, salE, and salF) from the S. albus ATCC 21838 and cloned them into the expression vector pWHM3. We demonstrated the noticeable expression and accumulation of trehalose, using only the five upstream biosynthetic gene cluster of salbostatin, in the transformed Streptomyces lividans TK24. Finally, 490 mg/l trehalose was produced by fermentation of the transformant with sucrosedepleted R2YE media.

Identification of Novel Irreversible Inhibitors of UDP-N-Acetylglucosamine Enolpyruvyl Transferase (MurA) from Haemophilus influenzae

  • Han, Seong-Gu;Lee, Won-Kyu;Jin, Bong-Suk;Lee, Ki-In;Lee, Hyeong Ho;Yu, Yeon Gyu
    • Journal of Microbiology and Biotechnology
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    • v.23 no.3
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    • pp.329-334
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    • 2013
  • Uridinediphospho-N-acetylglucosamine enolpyruvyl transferase (MurA, E.C. 2.5.1.7) is an essential bacterial enzyme that catalyzes the first step of the cell wall biosynthetic pathway, which involves the transfer of an enolpyruvyl group from phosphoenolpyruvate to uridinediphospho-Nacetylglucosamine. In this study, novel inhibitors of Haemophilus influenzae MurA (Hi MurA) were identified using high-throughput screening of a chemical library from the Korea Chemical Bank. The identified compounds contain a quinoline moiety and have much lower effective inhibitory concentrations ($IC_{50}$) than fosfomycin, a wellknown inhibitor of MurA. These inhibitors appear to covalently modify the sulfhydryl group of the active site cysteine (C117), since the C117D mutant Hi MurA was not inhibited by these compounds and excess dithiothreitol abolished their inhibitory activities. The increased mass value of Hi MurA after treatment with the identified inhibitor further confirmed that the active-site cysteine residue of Hi MurA is covalently modified by the inhibitor.

Mechanism Studies of Substituted Triazol-1-yl-pyrimidine Derivatives Inhibition on Mycobacterium tuberculosis Acetohydroxyacid Synthase

  • Chien, Pham Ngoc;Jung, In-Pil;Reddy, Katta Venugopal;Yoon, Moon-Young
    • Bulletin of the Korean Chemical Society
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    • v.33 no.12
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    • pp.4074-4078
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    • 2012
  • The first step in the common pathway for the biosynthesis of branched chain amino acids is catalyzed by acetohydroxyacid synthase (AHAS). The AHAS is found in plants, fungi and bacteria. With an aim to identify new anti-tuberculosis drugs that inhibit branched chain amino acid biosynthesis, we screened a chemical library against Mycobacterium tuberculosis AHAS. The screening identified four compounds, AVS 2087, AVS 2093, AVS 2236, and AVS 2387 with $IC_{50}$ values of 0.28, 0.21, 3.88, and $0.25{\mu}M$, respectively. Moreover, these four compounds also showed strong inhibition against reconstituted AHAS with $IC_{50}$ values of 0.37, 0.26, 1.0, and $1.18{\mu}M$, respectively. The basic scaffold of the AVS group consists of 1-pyrimidin-2-yl-1H-[1,2,4]-triazole-3-sulfonamide. The most active compound, AVS 2387, showed the lowest total interaction energy -8.75 Kcal/mol and illustrates its binding mode by hydrogen bonding with $H_{\varepsilon}$ of Gln517 with the distance of $2.24{\AA}$.

Genomewide Profiling of Rapamycin Sensitivity in Saccharomyces cerevisiae on Synthetic Medium

  • Chang, Yeon-Ji;Shin, Chun-Shik;Han, Dong-Hun;Kim, Ji-Yun;Kim, Kang-In;Kwon, Yong-Min;Huh, Won-Ki
    • Genomics & Informatics
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    • v.8 no.4
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    • pp.177-184
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    • 2010
  • The target of rapamycin (TOR) signaling pathway is a conserved pathway that regulates eukaryotic cell growth in response to environmental cues. Chemical genomic approaches that profile rapamycin sensitivity of yeast deletion strains have given insights into the function of TOR signaling pathway. In the present study, we analyzed the rapamycin sensitivity of yeast deletion library strains on synthetic medium. As a result, we identified 130 strains that are hypersensitive or resistant to rapamycin compared with wild-type cells. Among them, 36 genes are newly identified to be related to rapamycin sensitivity. Moreover, we found 16 strains that show alteration in rapamycin sensitivity between complex and synthetic media. We suggest that these genes may be involved in part of TOR signaling activities that is differentially regulated by media composition.