• 제목/요약/키워드: substrate inhibition

검색결과 448건 처리시간 0.024초

Inhibitory Effect of Benzoate-intercalated Hydrotalcite with Ce3+-loaded clay on Carbon Steel

  • Thuy Duong Nguyen;Thu Thuy Pham;Anh Son Nguyen;Ke Oanh Vu;Gia Vu Pham;To Thi Xuan Hang
    • Corrosion Science and Technology
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    • 제22권1호
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    • pp.1-9
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    • 2023
  • This work studied the inhibitory effect of the combination of benzoate-intercalated hydrotalcite (HT-BZ) and Ce3+-loaded clay (Clay-Ce) on carbon steel (CS). HT-BZ was prepared by the co-precipitation method and Clay-Ce was fabricated by a cation exchange reaction. HT-BZ and Clay-Ce were assessed by scanning electron microscopy (SEM) and X-ray diffraction (XRD) coupled with zeta potential measurement. Electrochemical measurements coupled with scanning electron microscopy/energy-dispersive X-ray spectroscopy (SEM/EDX) were used for studying the inhibitory action of the mixture of HT-BZ and Clay-Ce on steel electrodes immersed in 0.1 M NaCl. For comparison, the inhibitory effect of HT-BZ or Clay-Ce alone was also evaluated. The results showed that HT-BZ combined with Clay-Ce provided synergistic inhibition of the CS substrate. The mixture of 0.5 g/L HT-BZ + 0.5 g/L Clay-Ce provided 93.5% inhibition efficiency. The protective mechanism of the HT-BZ + Clay-Ce mixture consisted of the reaction of released BZ and Ce3+ and the deposition of HT-BZ and Clay-Ce structures on the CS substrate.

Site-directed Mutagenesis of Tyrosine 108 Residue in Human Glutathione S-Transferase P1-1

  • Ahn, So-Youn;Jeon, Sang-Hoon;Park, Hee-Joong;Kong, Kwang-Hoon
    • Bulletin of the Korean Chemical Society
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    • 제24권8호
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    • pp.1188-1192
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    • 2003
  • In order to study the role of residue in the active site of glutathione S-transferase (GST), Tyr 108 residue in human GST P1-1 was replaced with alanine, phenylalanine and tryptophan by site-directed mutagenesis to obtain mutants Y108A, Y108F and Y108W. These three mutant enzymes were expressed in Escherichia coli and purified to electrophoretic homogeneity by affinity chromatography on immobilized GSH. The substitutions of Tyr108 significantly affected $K_m^{CDNB}$ and $K_m^{ETA}$, whereas scarcely affected $K_m^{GSH}$. The substitutions of Tyr108 also significantly affected $I_{50}$ of ETA, an electrophilic substrate-like compound. The effect of these substitutions on kinetic parameters and the response to inhibition suggests that tyrosine 108 in hGST P1-1 contributes to the binding of the electrophilic substrate and a major determinant in the binding of CDNB is the aromatic ring of Tyr108, not its hydroxyl group.

Development of an Agar Diffusion Method to Measure Elastase Inhibition Activity Using Elastin-Congo Red

  • Jung Kyung-Hwan;Kim Hyun-Joo
    • Journal of Microbiology and Biotechnology
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    • 제16권8호
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    • pp.1320-1324
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    • 2006
  • The pancreatic and neutrophil elastases are associated with several illnesses including lung and vascular diseases, various cancers, and pancreatitis. The development of a potent and specific inhibitor to the elastases could lead to new therapies. In this study, an agar diffusion method was modified to include a substrate-dye conjugate (Elastin-Congo red) as a substrate of elastase and an indicator of elastase inhibitory activity. The Elastin-Congo red agar plates consisted of 0.1 % Elastin-Congo red and 2.5% agar. The elastase and elastase inhibitors were simultaneously loaded into wells, ultimately resulting in halo formations in which the halo diameter decreased as the concentration of elastase inhibitor increased. The concentration of elastase inhibitor in the samples, therefore, was inversely proportional to the halo diameters. This simplified method provided an excellent correlation with the standard microplate technique, which uses a chromogenic substrate. The concentration of elastase inhibitor obtained from the culture supernatant of a recombinant elastase inhibitor produced by the yeast Pichia pastoris was easily determined. This study has established a simple modified and inexpensive agar diffusion method that is potentially useful for the identification, quantification, and screening of new elastase inhibitors.

Inhibition of HIV-1 Pretense by Novel Dipeptide Isosteres Containing 2-Isoxazoline or $\alpha$-Hydroxy Ketomethylene

  • Kim, Do-Hyung;Park, Kwan-Yong;Chung, Yong-Jun;Kim, Byeang-Hyean
    • Biomolecules & Therapeutics
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    • 제2권2호
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    • pp.155-160
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    • 1994
  • Human immunodeficiency virus type 1 (HIV-1) protease is essential for the replication of the virus and it is therefore an attractive target for antiviral drugs of HIV-1. Several dipeptide isosteres containing 2-isoxazoline or $\alpha$-hydroxy ketomethylene have been synthesized and their inhibitory effects on the HIV-1 protease examined. The enzymatically active HIV-1 protease was purified to homogeniety from E. coli transformed with a recombinant plasmid (pMAL-pro) containing the entire gene encoding the protease. The purified protease had the substrate specificity with Km value of 9.8$\mu$M when an undecapeptide His-Lys-Ala-Arg-Val-Leu-(p-nitro)Phe-Glu-Ala-Nle-Ser-amide was used as a substrate, and the products from the substrate after specific cleavage by HIV-1 protease were analyzed by HPLC. The synthetic compounds containing dipeptide isosteres showed specific inhibitory effects while a dipeptide isostere containing an isoxazoline ring inhibited the HIV-1 protease competitively with Ki value of 500 $\mu$M. Even if the inhibition effects of HIV-1 protease were not very high, these novel dipeptide isosteres can be used as key structural moieties for developing specific inhibitors of HIV-1 protease.

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양배추 유래의 글루타티온 전달효소의 기질 특이성 및 저해 효과 분석 (Analysis on the substrate specificity and inhibition effect of Brassica oleracea glutathione S-Transferase)

  • 박희중;이희진;공광훈
    • 분석과학
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    • 제22권3호
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    • pp.228-234
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    • 2009
  • 본 연구에서는 식물의 제초제 해독 기구를 알아보기 위해, 양배추 (Brassica oleracea)로 부터 글루타티온 전달효소를 정제하고 외래성 이물질에 대한 기질 특이성과 저해 효과를 분석하였다. 양배추로부터 DEAE-Sephacel 컬럼과 GSH-Sepharose 컬럼 크로마토그래피를 이용하여 약 10%의 수율로 글루타티온 전달효소를 정제하였다. 정제된 효소에 대해 분자량을 측정한 결과, SDS-polyacrylamide 겔 전기영동으로 측정한 분자량은 23,000Da을 나타내었으며, 겔 크로마토그래피로 측정한 분자량은 48,000Da을 나타내었다. 따라서 정제된 양배추 글루타티온 전달효소는 소단위체의 분자량이 약 23,000Da의 동종이량체라는 사실을 알 수 있었다. 이 효소의 저해제에 대한 효과를 조사한 결과, S-hexyl-GSH와 S-(2,4-dinitrophenyl)GSH에 의해 활성이 저해되었다. 양배추 글루타티온 전달효소의 기질특이성은 CDNB와 ETA에서 높은 활성을 보였으며, cumene hydroperoxide에 대한 GSH peroxidase 활성도 나타내었다.

효소공정에 의한 트립토판 생산 (Production of L-Tryptophan by Enzymatic Processes)

  • 이인영;안경섭;김의환;이선복
    • 한국미생물·생명공학회지
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    • 제20권1호
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    • pp.73-78
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    • 1992
  • Tryptophanase를 이용하여 트립토판 합성시 인돌의 효소활성 저해를 억제하기 위하여 유가식 조업, 유기용매 이상계의 사용, 그리고 cyclodextrin의 첨가등에 대하여 연구하였다. 효소 농도가 0.5mg/ml일때 인돌 농도 0.4mM 부근에서 트립토판 생성이 가장 빨랐으며 그 이상에서는 효소활성이 심한 저해를 받았다. 초기 인돌 농도가 20mM일 때는 27시간 반응후 인돌의 전환율이 20인데 비하여 반응기내 인돌 농도를 5mM 이하로 유가식 조업을 하였을 때 전환율이 80%로 향상되었다.

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후지 사과 Polyphenol Oxidase의 특성 및 활성억제 (Characteristics and Inhibition of Polyphenol Oxidase from Fuji Apples)

  • 최언호;정동선;조남숙;심영현
    • Applied Biological Chemistry
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    • 제30권3호
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    • pp.278-284
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    • 1987
  • 사과의 건조, 가공 중의 갈변을 방지하기 위한 기초 조사로서 후지 사과로부터 추출한 crude polyphenol oxidase의 특성과 열에 대한 저항성, 갈변 저해제의 저해 효과 등을 조사하였다. Catechol을 기질로 사용하였을 때 polyphenol oxidase의 최적 pH는 5.5, 최적온도는 $20^{\circ}C$, $K_m$ 값은 0.14M이었고, 열불활성화는 유사일차반응을 보였으며 이때 활성화에너지$(E_a)$와 Z값은 각각 23.0cal/kmol, $19.7^{\circ}C$였다. 기질에 따른 친화력은 o-diphenol, 특히 chlorogenic acid에 대하여 높았고, monophenol과 m-diphenol, p-diphenol에 대해서는 나타나지 않았다. Polyphenol oxidase에 의한 갈변은 thiourea와 potassium metabisulfite는 10mM에서, L-cysteine과 ascorbic acid, sodium diethyldithiocarbamate는 1mM에서 현저하게 저해되었다.

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수종 모노테르펜계 화합물이 랫드 뇌의 monoamine oxidase활성에 미치는 영향 (Effects of Some Monoterpenes on Rat Brain Monoamine Oxidase)

  • 문창규;임종석;유충규
    • 한국식품위생안전성학회지
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    • 제10권4호
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    • pp.279-282
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    • 1995
  • Eight natural or semistynthesized monoterpenes were examined for their effects in rat brain monoamine oxidase(MAO) using benzylamine as substrate. Thujone and 3-carene were found to have the inhibition effects on rat brain MAQ activity, 38% and 95% inhibition at 103M respectively. The kinetic study on 3-carene, the most potent inhibitive type. But (+) pulegon and (-) isopulegon was found to activate MAO slightly.

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온도와 초기 BTEX농도변화에 따른 BTEX 분해특성

  • 장순웅;라현주;이시진
    • 한국지하수토양환경학회:학술대회논문집
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    • 한국지하수토양환경학회 1999년도 추계학술발표회
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    • pp.19-22
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    • 1999
  • A microbial consortium derived from a gasoline-contaminated sites was enriched on toluene in 100-mL serum bottle and was found to degrade benzene(B), toluene(T), ethylbenzene(EB), and xylenes(X). Studies conducted to determine the temperature effects and BTEX concentration on BTEX degradation. The results indicated that lowering temperature significantly decreased BTEX degradation rates and varing the BTEX concentration also changed substrate degradation patterns.

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Rigorous Model for Spherical Cell-support Aggregate

  • Moon, Seung-Hyeon;Lee, Ki-Beom;Satish J. Paruekar
    • Biotechnology and Bioprocess Engineering:BBE
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    • 제6권1호
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    • pp.42-50
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    • 2001
  • The activity of immobilized cell-support particle aggregates is influenced by physical and biochemical elements, mass transfer, and physiology. Accordingly, the mathematical model discussed in this study is capable of predicting the steady state and transient concentration profiles of the cell mass and substrate, plus the effects of the substrate and product inhibition in an immobilized cell-support aggregate. The overall mathematical model is comprised of material balance equations for the cell mass, major carbon source, dissolved oxygen, and non-biomass products in a bulk suspension along with a single particle model. A smaller bead size and higher substrate concentration at the surface of the particle, resulted in a higher supply of the substrate into the aggregate and consequently a higher biocatalyst activity.

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