• Title/Summary/Keyword: Combinatorial library

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Synthesis and Photoluminescence Properties of Y1-x(P1-y-zNbyVz)O4:Eux Phosphors by Modified Combinatorial Chemistry Method (조합화학 기법을 이용한 Y1-x(P1-y-zNbyVz)O4:Eux 형광체의 합성 및 빛 발광 특성)

  • Zeon, Il-Woon;Sohn, Kee-Sun;Park, Hee-Dong
    • Journal of the Korean Chemical Society
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    • v.46 no.1
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    • pp.69-75
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    • 2002
  • The $Y_{1-x}(P_{1-y-z}Nb_yV_z)O_4:Eu_x$ blue and red emitting phosphors were prepared by the combinatorial chemistry method. The combinatorial library was designed to investigate the luminescence of the $Y_{1-x}(P_{1-y-z}Nb_yV_z)O_4:Eu_x$ phosphors under 254 nm and 147 nm excitations. In addition, the crystallinity and morphology of phosphors were checked by XRD and SEM. Based on the results from the combinatorial screenings, luminescent properties of phosphors are strongly dependent on the concentration of doping metal ions. It was found that a new phosphor $Y_{0.88}(P_{0.92}Nb_{0.05}V_{0.03})O_4:Eu_{0.12}$ shows excellent luminescent efficiency comparing to the $Y_{0.88}PO_4:Eu_{0.12}$ red phosphor.

Inhibition of the Replication of Hepatitis C Virus Replicon with Nuclease-Resistant RNA Aptamers

  • Shin, Kyung-Sook;Lim, Jong-Hoon;Kim, Jung-Hye;Myung, Hee-Joon;Lee, Seong-Wook
    • Journal of Microbiology and Biotechnology
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    • v.16 no.10
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    • pp.1634-1639
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    • 2006
  • Hepatitis C virus (HCV)-encoded nonstructural protein 5B (NS5B) possesses RNA-dependent RNA polymerase activity, which is considered essential for viral proliferation. Thus, HCV NS5B is a good therapeutic target protein for the development of anti-HCV agents. In this study, we isolated two different kinds of nuclease-resistant RNA aptamers with 2'-fluoro pyrimidines against the HCV NS5B from a combinatorial RNA library with 40 nucleotide random sequences, using SELEX technology. The isolated RNA aptamers were observed to specifically and avidly bind the HCV NS5B with an apparent $K_d$ of 5 nM and 18 nM, respectively, in contrast with the original RNA library that hardly bound the target protein. Moreover, these aptamers could partially inhibit RNA synthesis of the HCV subgenomic replicon when transfected into Huh-7 hepatoma cell lines. These results suggest that the RNA aptamers selected in vitro could be useful not only as therapeutic agents of HCV infection but also as a powerful tool for the study of the HCV RNA-dependent RNA polymerase mechanism.

Synthesis of Silicon Tracelsss Linker for Solid-Phase Reaction

  • Mun Han-Seo;Seong Jin-Hyun
    • Archives of Pharmacal Research
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    • v.27 no.4
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    • pp.371-375
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    • 2004
  • The silicon linker is the foremost traceless linker used in solid-phase reactions. Hydrogen fluo-ride (HF) or trifluoroacetic aicd (TFA) can remove the silicon linker with the silicon atom being replaced by a hydrogen atom. In this experiment, the linkers 1c and 2d, which are the most useful in solid-phase reactions, were synthesized, Linker 1c is composed of seven linearly linked carbons and linker 2d includes an oxygen atom in the linear carbon chain to increase the solvation capacity. The carboxylic acid component of linker 1c and 2d forms an amide or ester bond with resin. The synthesized linkers 1c and 2d could be utilized in constructing a chemical compound library that includes indole, benzodiazepine and phenothiazine (aromatic ring compounds).

Implementation of Systolic Array for the Single-Source Shortest Path Problem

  • Lee, Jae-Jin;Park, Jeong-Pil;Hwang, In-Jae;Song, Gi-Yong
    • Proceedings of the IEEK Conference
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    • 2002.07a
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    • pp.361-364
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    • 2002
  • Shortest path problem belongs to the combinatorial optimization problem and plays an important role in the field of computer aided design. It can either be directly applied as in the case of routing or serves as a important subroutine in more complex problems. In this paper, a systolic array for the SSSP(single-source shortest path problem) was derived. The array was modeled and simulated in RTL level using VHDL, then synthesized to a schematic and finally implemented to a layout using the cell library based on 0.35 $\mu\textrm{m}$ CMOS 1-poly 4-metal CMOS technology.

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신약개발 환경의 변화와 대응책

  • 유성은
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2000.04a
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    • pp.1-2
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    • 2000
  • 일반적인 신약 개발 방법으로는 천연물로부터 선도화합물이 발견되었을 때 의약화학자들은 그 물질의 화학구조식 중에서 약리 작용에 필수 요건이 되는 구조 요소를 규정하고, 체계적인 분자변형을 통하여 약리 작용의 최적화 작업을 추진한다. 그러나 분자 내에 여러 가지 치환기를 도입할 수 있는 경우 수많은 유도체가 합성 가능하며, 실제로 이와 같은 많은 수의 유도체를 합성한다는 것은 현실적으로 불가능하다. 통계적으로 하나의 신약 개발에 드는 시간과 경비는 약 10년 이상의 기간과 3,000 억원 이상의 경비가 소요된다. 따라서 시간과 경비를 줄이는 노력의 하나로 실험분야에서는 조합 화학합성 (Combinatorial Chemical Synthesis, CCS) 기술인 새로운 개념의 고효율 합성 기술이나 이를 대량 검색할 수 있는 초고속 활성 검색법 (High Through-put Screening, HTS) 기술이 1990년대 초에 본격적으로 각광 받게되었고, 정보관리 시스템을 통한 library 구축, 컴퓨터를 이용한 구조-활성 관계 및 분자 설계 기법이 급속히 발전하게 되었다. 따라서 기존의 random screening에 의한 신약개발 방법으로부터 탈피하여 새로운 차원의 신의약 개발 방법의 필요성이 절실히 요구되고 있다.

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An Integer Programming-based Local Search for the Set Partitioning Problem

  • Hwang, Junha
    • Journal of the Korea Society of Computer and Information
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    • v.20 no.9
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    • pp.21-29
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    • 2015
  • The set partitioning problem is a well-known NP-hard combinatorial optimization problem, and it is formulated as an integer programming model. This paper proposes an Integer Programming-based Local Search for solving the set partitioning problem. The key point is to solve the set partitioning problem as the set covering problem. First, an initial solution is generated by a simple heuristic for the set covering problem, and then the solution is set as the current solution. Next, the following process is repeated. The original set covering problem is reduced based on the current solution, and the reduced problem is solved by Integer Programming which includes a specific element in the objective function to derive the solution for the set partitioning problem. Experimental results on a set of OR-Library instances show that the proposed algorithm outperforms pure integer programming as well as the existing heuristic algorithms both in solution quality and time.

Facile Synthesis of 3-Thioxo-3H-benzo[f]chromen-2-yl methanone and 3H-Benzo[f]chromene-3-one Under Solvent Free Condition

  • Singh, Okram Mukherjee;Devi, Nepram Sushuma;Devi, Laishram Ronibala;Lim, Ki-Bum;Yoon, Yong-Jin;Lee, Sang-Geyong
    • Bulletin of the Korean Chemical Society
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    • v.32 no.1
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    • pp.175-178
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    • 2011
  • A facile, convenient, efficient and high yielding synthesis of a combinatorial library of coumarins has been developed by the condensation of readily available $\beta$-oxodithioesters and S,S-acetal with 2-hydroxy-1-naphthaldehyde in the presence of catalytic amount of $CuCl_2$ under solvent free conditions.

Design and Implementation of the Systolic Array for Dynamic Programming

  • Lee, Jae-Jin;Tien, David;Song, Gi-Yong
    • Journal of the Institute of Convergence Signal Processing
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    • v.4 no.3
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    • pp.61-67
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    • 2003
  • We propose a systolic array for dynamic programming which is a technique for solving combinatorial optimization problems. We derive a systolic array for single source shortest path Problem, SA SSSP, and then show that the systolic array serves as dynamic Programming systolic array which is applicable to any dynamic programming problem by developing a systolic array for 0 1 knapsack problem, SA 01KS, with SA SSSP for a basis. In this paper, each of SA SSSP and SA 01KS is modeled and simulated in RT level using VHDL, then synthesized to a schematic and finally implemented to a layout using the cell library based on 0.35${\mu}{\textrm}{m}$ 1 poly 4 metal CMOS technology.

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Design, Combinatorial Library Synthesis and Biological Evaluation of Nonpeptide Scaffold for Beta Turns

  • Im, I-Sak;Thomas R.Webb;Dona Chianelli;Kim, Yong-Chul
    • Proceedings of the PSK Conference
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    • 2003.10a
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    • pp.91-91
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    • 2003
  • The beta-turn has been implicated as an important conformation for biological recognition of peptides or proteins. We adapted the concept of general Ca atom positioning from the cluster analysis and recombination of each ideal beta-turn conformation pattern by Garland and Dean (1. Computer-Aided Molecular Design, 1999, 13, 469) as one strategy of designing non-peptide beta-turn scaffolds. (omitted)

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Efficient Target Site Selection for an RNA-cleaving DNAzyme through Combinatorial Library Screening

  • Kim, Ki-Sun;Choi, Woo-Hyung;Gong, Soo-Jeong;Oh, Sang-taek;Kim, Jae-Hyun;Kim, Dong-Eun
    • Bulletin of the Korean Chemical Society
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    • v.27 no.5
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    • pp.657-662
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    • 2006
  • Identification of accessible sites in targeted RNAs is a major limitation to the effectiveness of antisense oligonucleotides. A class of antisense oligodeoxynucleotides, known as the “10-23” DNA enzyme or DNAzyme, which is a small catalytic DNA, has been shown to efficiently cleave target RNA at purine-pyrimidine junctions in vitro. We have designed a strategy to identify accessible cleavage sites in the target RNA, which is hepatitis C virus nonstructural gene 3 (HCV NS3) RNA that encodes viral helicase and protease, from a pool of random DNAzyme library. A pool of DNAzymes of 58 nucleotides-length that possess randomized annealing arms, catalytic core sequence, and fixed 5'/3'-end flanking sequences was designed and screened for their ability to cleave the target RNA. The screening procedure, which includes binding of DNAzyme pool to the target RNA under inactive condition, selection and amplification of active DNAzymes, incubation of the selected DNAzymes with the target RNA, and target site identification on sequencing gels, identified 16 potential cleavage sites in the target RNA. Corresponding DNAzymes were constructed for the selected target sites and were tested for RNA-cleavage in terms of kinetics and accessibility. These selected DNAzymes were effective in cleaving the target RNA in the presence of $Mg^{2+}$. This strategy can be applicable to identify accessible sites in any target RNA for antisense oligonucleotides-based gene inactivation methods.