• Title/Summary/Keyword: linker

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Construction of Indole Library for Serotonin Related Drugs and Macrocyclization Using Selenium Chemistry in Solid-Phase Reaction.

  • Mun, Han-Seo;Jeong, Jin-Hyun
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.246.1-246.1
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    • 2003
  • Hetero chain compounds have high possibilities of being good medicinal candidate because of their well-known medicinal activity and relatively low subtitled carbon. By constructing the method of making this compound library, this research has the purpose to create a new medicinal candidate materials based on an easy medicinal search. The first step is to construct an Indole library in a compounding process with the design of a linker connecting a solid-state resin and a substrate. (omitted)

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InP Quantum Dot-Organosilicon Nanocomposites

  • Dung, Mai Xuan;Mohapatra, Priyaranjan;Choi, Jin-Kyu;Kim, Jin-Hyeok;Jeong, So-Hee;Jeong, Hyun-Dam
    • Bulletin of the Korean Chemical Society
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    • v.33 no.5
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    • pp.1491-1504
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    • 2012
  • InP quantum dot (QD)-organosilicon nanocomposites were synthesized and their photoluminescence quenching was mainly investigated because of their applicability to white LEDs (light emitting diodes). The as-synthesized InP QDs are capped with myristic acid (MA), which are incompatible with typical silicone encapsulants. We have introduced a new ligand, 3-aminopropyldimethylsilane (APDMS), which enables embedding the QDs into vinyl-functionalized silicones through direct chemical bonding. The exchange of ligand from MA to APDMS does not significantly affect the UV absorbance of the InP QDs, but quenches the PL to about 10% of its original value with the relative increase in surface related emission intensities, which is explained by stronger coordination of the APDMS ligands to the surface indium atoms. InP QD-organosilicon nanocomposites were synthesized by connecting the QDs using a short cross-linker such as 1,4-divinyltetramethylsilylethane (DVMSE) by the hydrosilylation reaction. The formation and changes in the optical properties of the InP QD-organosilicon nanocomposite were monitored by ultraviolet visible (UV-vis) absorbance and steady state photoluminescence (PL) spectroscopies. As the hydrosilylation reaction proceeds, the QD-organosilicon nanocomposite is formed and grows in size, causing an increase in the UV-vis absorbance due to the scattering effect. At the same time, the PL spectrum is red-shifted and, very interestingly, the PL is quenched gradually. Three PL quenching mechanisms are regarded as strong candidates for the PL quenching of the QD nanocomposites, namely the scattering effect, F$\ddot{o}$rster resonance energy transfer (FRET) and cross-linker tension preventing the QD's surface relaxation.

Transfer and Expression of the Recombinant hFSH Gene in CHO Cells and Transgenic Chickens using Retrovirus Vector System (CHO 세포와 형질전환 닭에 있어서 Retrovirus Vector System에 의한 hFSH 재조합 유전자의 전이와 발현)

  • 권모선;구본철;심호섭;박창식;이성호;김태완
    • Korean Journal of Animal Reproduction
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    • v.27 no.3
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    • pp.197-206
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    • 2003
  • hFSH (human follicle stimulating hormone) is heterodimer consisting of $\alpha$ and $\beta$ subunits. Since assembly of the both subunits in the cell is often the rate-limiting step in production of functional hormone, single-chain hormones have been engineered by genetically linking two different cDNA fragments with a linker sequence. Using retrovirus vector system, the resulting recombinant hFSH gene was transferred in CHO cells and chicken embryos, and the expression of the gene was investigated. In CHO cells, protein synthesis from the single-chain FSH gene was 17 fold higher than that from the heterodimeric counterpart. In the study of transgenic chickens, ten of the eleven chicks hatched from 62 embryos manupulated with recombinant retrovirus stock was determined to carry transgenic genes. RT-PCR analyses confirmed transcription of the single-chain FSH gene, however, no recombinant FSH was detected from the blood samples.

The Implementation of C Cross-Compiler for ES-C2340 DSP2 by Using the GNU Compiler (GNU 컴파일러를 이용한 ES-C2340 DSP2용 C 교차 컴파일러의 개발)

  • Lee, Si-Yeong;Gwon, Yuk-Chun;Yu, Ha-Yeong;Han, Gi-Cheon;Kim, Seung-Ho
    • The Transactions of the Korea Information Processing Society
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    • v.4 no.1
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    • pp.255-269
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    • 1997
  • In this paper, we describe the implementation of C cross-compiler for the ES-C2340 DSP2 processor by using the GNU compiler. For the rapid and efficient developing of the compiler and other parts like the processor-dependent back -end which is implemented newly to build the compiler. This approach has several advantages. First, as we use GNU compiler's well-proved excellent optimization method and multi-language support capability, we can improve he efficiency and generality of the compiler. Second, as we concentrate on the high-level language as logic approving tool in processor developing process. And to support the cross-compiler, we also implement a text-level pre-linker.

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Improving the Productivity of Single-Chain Fv Antibody Against c-Met by Rearranging the Order of its Variable Domains

  • Kim, Yu-Jin;Neelamegam, Rameshkumar;Heo, Mi-Ae;Edwardraja, Selvakumar;Paik, Hyun-Jong;Lee, Sun-Gu
    • Journal of Microbiology and Biotechnology
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    • v.18 no.6
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    • pp.1186-1190
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    • 2008
  • Single-chain Fv (scFv) antibody against c-Met is expected to be employed in clinical treatment or imaging of cancer cells owing to the important biological roles of c-Met in the proliferation of malignancies. Here, we show that the productivity of scFv against c-Met in Escherichia coli is significantly influenced by the orientation of its variable domains. We generated anti-c-Met scFv antibodies with two different domain orders (i.e., $V_L$-linker-$V_H$ and $V_H$-linker-$V_L$), expressed them in the cytoplasm of E. coli trx/gor deleted mutant, and compared their specific activities as well as their productivities. Productivity of total and functional anti-c-Met scFv with $V_H/V_L$ orientation was more than five times higher than that with $V_L/V_H$ format. Coexpression of DsbC enhanced the yield of soluble amounts of anti-c-Met scFv protein for both constructs. The purified scFv antibodies of the two different formats exhibited almost the same antigen-binding activities. We also compared the productivities and specific activities of anti-c-Met diabodies with $V_H/V_L$ or $V_L/V_H$ formats and obtained similar results to the case of scFv antibodies.

Oxidation-Induced Conformational Change of a Prokaryotic Molecular Chaperone, Hsp33, Monitored by Selective Isotope Labeling

  • Lee, Yoo-Sup;Ryu, Kyoung-Seok;Lee, Yuno;Kim, Song-Mi;Lee, Keun-Woo;Won, Hyung-Sik
    • Journal of the Korean Magnetic Resonance Society
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    • v.15 no.2
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    • pp.137-145
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    • 2011
  • Hsp33, a prokaryotic molecular chaperone, exerts holdase activity in response to oxidative stress. In this study, the stepwise conformational change of Hsp33 upon oxidation was monitored by NMR. In order to overcome its high molecular weight (33 kDa as a monomer and 66 kDa as a dimer), spectra were simplified using a selectively [$^{15}N$]His-labeled protein. All of the eight histidines were observed in the TROSY spectrum of the reduced Hsp33. Among them, three peaks showed dramatic resonance shifts dependent on the stepwise oxidation, indicating a remarkable conformational change. The results suggest that unfolding of the linker domain is associated with dimerization, but not entire region of the linker domain is unfolded.

DNA Structural Perturbation Induced by the CPI-Derived DNA Interstrand Cross-linker : Molecular Mechanisms for the Sequence Specific Recognition

  • Park, Hyun-Ju
    • Archives of Pharmacal Research
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    • v.24 no.5
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    • pp.455-465
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    • 2001
  • The highly potent cytotoxic DNA-DNA cross-linker consists of two cyclopropa[c]pyrrolo[3,4-3]indol-4(5H)-ones insoles [(+)-CPI-I] joined by a bisamido pyrrole (abbreviated to "Pyrrole"). The Pyrrole is a synthetic analog of Bizelesin, which is currently in phase II clinical trials due to its excellent in vivo antitumor activity. The Pyrrole has 10 times more potent cytotoxicity than Bizelesin and mostly form DNA-DNA interstrand cross-links through the N3 of adenines spaced 7 bp apart. The Pyrrole requires a centrally positioned GC base pair for high cross-linking reactivity (i.e., $5^1$-T$AT_2$A*-$3^1$), while Bizelesin prefers purely AT-rich sequences (i.e., $5^1$-T$AT_4$A*-$3^1$, where /(equation omitted) represents the cross-strand adenine alkylation and A* represents an adenine alkylation) (Park et al., 1996). In this study, the high-field $^1$H-NMR and rMD studies are conducted on the 1 1-mer DNA duplex adduct of the Pyrrole where the 5′(equation omitted)TAGTTA*-3′sequence is cross-linked by the drug. A severe structural perturbation is observed in the intervening sequences of cross-linking site, while a normal B-DNA structure is maintained in the region next to the drug-modified adenines. Based upon these observations, we propose that the interplay between the bisamido pyrrole unit of the drug and central C/C base pair (hydrogen-bonding interactions) is involved in the process of cross-linking reaction, and sequence specificity is the outcome of those interactions. This study suggests a mechanism for the sequence specific cross-linking reaction of the Pyrrole, and provides a further insight to develop new DNA sequence selective and distortive cross-linking agents.

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Analysis of Porcine $\beta$-casein Gene Promoter by Site-directed Mutagenesis

  • Chung, Hee-Kyoung;Seong, Hwan-Hoo;Im, Seok-Ki;Lee, Hyun-Gi;Kim, Soon-Jeung;Lee, Poongyeong;Lee, Yun-Keun;Chang, Won-Kyong;Moosik Kwon
    • Proceedings of the Korean Society of Embryo Transfer Conference
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    • 2002.11a
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    • pp.71-71
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    • 2002
  • Promoters for milk proteins have been used far producing transgenic animals due to their temporal and spatial expression patterns. ${\beta}$-casein, a calcium-sensitive casein, is a major milk protein that corresponds ca. 30 per cent of total milk protein. Expression of ${\beta}$-casein is controlled by lactogenic hormones such as prolactin (PRL), composite response elements (CoREs) and transcription factors. CoREs are clusters of transcription factor binding sites containing both positive and negative regulatory elements. ${\beta}$-casein gene promoter contains various regions (CoREs) for gene transcription. We analyzed the promoter region by mutagenesis using exonuclease III and linker-scanning. Transcription control elements usually are positioned in 5'-flanking region of the gene. However, in some cases, these elements are located in other regions such as intron 1. The nucleotide sequences of ${\beta}$-casein promote. region has been reported (E12614). However, the properties of the promoter is not yet clear. In this study, we plan to investigate the properties of cis-regulating elements of porcine ${\beta}$-casein by mutation analysis and expression analysis using dual-luciferase repoter assay system.

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Conjugation of Ginsenoside Rg3 with Gold Nanoparticles

  • Park, You-Mie;Im, A-Rang;Joo, Eun-Ji;Lee, Ji-Hye;Park, Hyeung-Geun;Kang, Young-Hwa;Linhardt, Robert J.;Kim, Yeong-Shik
    • Bulletin of the Korean Chemical Society
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    • v.32 no.1
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    • pp.286-290
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    • 2011
  • Ginsenoside Rg3 was reported to have important biological activities. We demonstrate conjugation and quantification procedures of ginsenoside Rg3 to gold nanoparticles for future biological and medical applications. Ginsenoside Rg3 was conjugated to spherical gold nanoparticles using a bifunctional heptaethylene glycol linker. The sulfhydryl group of heptaethylene glycol was adsorbed onto gold nanoparticles, and carboxylic acid end of heptaethylene glycol was bonded through a hydroxyl group of Rg3 via ester bond formation. The conjugation of Rg3 was characterized with various spectroscopic techniques, high resolution-transmission electron microscopy, and using Rg3 monoclonal antibody. The Rg3- functionalized gold nanoparticles were $4.7{\pm}1.0$ nm in diameter with a surface charge of -4.12 mV. The total number of Rg3 molecules conjugated to a 3.6 mL solution of gold nanoparticle was determined to be $9.5{\times}10^{14}$ corresponding to ~6 molecules of Rg3/gold nanoparticle. These results suggest that ginsenoside Rg3 is successfully conjugated to gold nanoparticles via heptaethylene glycol linker. The quantification was performed by using Rg3 monoclonal antibody without interference of gold's intrinsic color.

Direct characterization of E2-dependent target specificity and processivity using an artificial p27-linker-E2 ubiquitination system

  • Ryu, Kyoung-Seok;Choi, Yun-Seok;Ko, Jun-Sang;Kim, Seong-Ock;Kim, Hyun-Jung;Cheong, Hae-Kap;Jeon, Young-Ho;Choi, Byong-Seok;Cheong, Chae-Joon
    • BMB Reports
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    • v.41 no.12
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    • pp.852-857
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    • 2008
  • Little attention has been paid to the specificity between E2 and the target protein during ubiquitination, although RING-E3 induces a potential intra-molecular reaction by mediating the direct transfer of ubiquitin from E2 to the target protein. We have constructed artificial E2 fusion proteins in which a target protein (p27) is tethered to one of six E2s via a flexible linker. Interestingly, only three E2s (UbcH5b, hHR6b, and Cdc34) are able to ubiquitinate p27 via an intra-molecular reaction in this system. Although the first ubiquitination of p27 (p27-Ub) by Cdc34 is less efficient than that of UbcH5b and hHR6b, the additional ubiquitin attachment to p27-Ub by Cdc34 is highly efficient. The E2 core of Cdc34 provides specificity to p27, and the residues 184-196 are required for possessive ubiquitination by Cdc34. We demonstrate direct E2 specificity for p27 and also show that differential ubiquitin linkages can be dependent on E2 alone.