• Bulletin of the Korean Chemical Society
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• 제35권5호
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• pp.1269-1274
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• 2014

Monoamine oxidases catalyze the oxidative deamination of dietary amines and amine neurotransmitters, and assist in maintaining the homeostasis of the amine neurotransmitters in the brain. Dysfunctions of these enzymes can cause neurological and behavioral disorders including Parkinson's and Alzheimer's diseases. To understand their physiological roles, efficient assay methods for monoamine oxidases are essential. Reviewed in this Perspective are the recent progress in the development of fluorescent probes for monoamine oxidases and their applications to enzyme assays in cells and tissues. It is evident that still there is strong need for a fluorescent probe with desirable substrate selectivity and photophysical properties to challenge the much unsolved issues associated with the enzymes and the diseases.

• BMB Reports
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• 제44권9호
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• pp.559-565
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• 2011

Protein kinase C (PKC) is a central enzyme that modulates numerous biological functions. For this reason, specific PKC inhibitors/activators are required to study PKC-related signaling mechanisms. To date, although many PKC inhibitors have been developed, they are limited by poor selectivity and nonspecificity. In this review, we focus on the nonspecific actions of PKC inhibitors on cardiovascular ion channels in addition to their PKC-inhibiting functions. The aim of this paper is to urge caution when using PKC inhibitors to block PKC function. This information may help to better understand PKC-related physiological/biochemical studies.

• KSBB Journal
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• 제13권1호
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• pp.38-43
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• 1998

Application of pervaporative extraction of ethanol to simultaneous saccharification and fermentation(SSF) of cellulose was investigated. From batch experiments, optimum cellulose substrate and enzyme loadings were found to be 10% and 15 IFPU/g cellulose, respectively. The cellulose conversion was lowered in fed-batch system due to the ethanol accumulation. The activity of the yeast Saccharomyces uvarum used in this study was significantly reduced at ethanol concentrations above around 40 g/L. From pervaporation experiments using PDMS membrane, ethanol was efficiently separated at 38$^\circ C$ and 10 mmHg of a down stream pressure. The pervaporation unit with 240 cm$^2$ of surface area was combined into the SSF reactor. The continuous removal of ethanol by pervaporation during SSF resulted in an improved cellulose conversion. Within the scope of this experiment, ethanol yields in the pervaporative SSF and simple SSF were 68.3% and 56.6%, respectively. The permeate flux for SSF broth pervaporation was about one-half that for the pervaporation of aqueous ethanol solution. Accordingly, the development of a membrane with higher ethanol selectivity and flux will increase the feasibility of this technology.

• 대한안전경영과학회지
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• 제1권1호
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• pp.259-272
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• 1999

In order to enhance the selectivity, productivity and yield of methyl fructoside, which was synthesized by enzymatic glycosylation of sucrose and methanol solution, controlling of surface property of solid support using different immobilization procedures optimized microenvironment of immobilized invertase. Silanization and polyethylene imine coating methods were adopted to give a hydrophobic and hydrophilic environment of immobilized invertase. As a result, polyethyleneimine coating method gave higher loading of enzyme, effective activity, and relative activity than silanization method, because it brought on increasing the functional density of amino group and enhancing the conservation of activity by regulating of hydrophilicity. And then, hydrophilic environment was possible to restraint the assessing of methyl fructoside molecule, which was more hydrophobic than sucrose, fructose, and glucose molecule in the reaction mixture, into .the active site of immobilizedinvertase. Consequently, hydrophilic microenvironment of immobilized invertase by polyethyleneimine coating obtained higher yield and productivity with increasing conversion than silanized and native invertase. Thus, this procedure optimized the microenvironment of immobilized invertase suitable for the enzymatic synthesis of methyl fructoside.

• Bulletin of the Korean Chemical Society
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• 제24권3호
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• pp.291-294
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• 2003

A highly interferent-resistive membrane, poly-5-amino-1-naphthol (poly-5A1N), underlied beneath enzymeembedded poly-1,3-phenylendiamine (poly-m-PD) network for miniturized continuous monitoring glucose sensors. The enzyme layer was prepared from a mixed solution of glucose oxidase (GOx) and m-PD monomer by simple electrolysis. The mass change of poly-5A1N was monitored by electrochemical quartz crystal microbalance (EQCM) in situ and the corresponding thickness was measured. Successive electropolymerization of poly-5A1N and poly-m-PD create a several tens nm-thick bilayer showing excellent selectivity for $H_2O_2$ and low activity loss of immobilized enzymes.

• Bulletin of the Korean Chemical Society
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• 제31권6호
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• pp.1568-1572
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• 2010

The selective isolation of specific proteins from complex protein mixtures by nanoparticles is reported. Glutathionemodified superparamagnetic nanoparticles were used to purify specific proteins fused with glutathione S-transferase via enzyme-substrate interactions. They demonstrated greatly improved selectivity and efficiency over micron sized capturing beads. The ultra-specific enrichment of target proteins was confirmed by both SDS-PAGE and LC/MS/MS experiments.

• Archives of Pharmacal Research
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• 제22권6호
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• pp.533-541
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• 1999

Many conventional anticancer drugs display relatively poor selectivity for neoplastic cells, in particular for solid tumors. Furthermore, expression or development of drug resistance, increased glutathione transferases as well as enhanced DNA repair decrease the efficacy of these drugs. Research efforts continue to overcome these problems by understanding these mechanisms and by developing more effective anticancer drugs. Cyclophosphamide is one of the most widely used alkylating anticancer agents. Because of its unique activation mechanism, numerous bioreversible prodrugs of phosphramide mustard, the active species of cyclophosphamide, have been investigated in an attempt to improve the therapeutic index. Solid tumors are particularly resistant to radiation and chemotherapy. There has been considerable interest in designing drugs selective for hypoxic environments prevalent in solid tumors. Much of the work had been centered on nitroheterocyclics that utilize nitroreductase enzyme systems for their activation. In this article, recent developments of anticancer prodrug design are described with a particular emphasis on exploitation of selective metabolic processes for their activation.

• KSBB Journal
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• 제19권2호
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• pp.164-167
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• 2004

효소인 싸이클로덱스트린글루카노트란스퍼라제 (CGTase)는 효소의 활성도에 칼슘이 관련된 분자내 당 전이반응에 의해 녹말과 그에 관련된 $\alpha$-1,4-glucan의 기질을 싸이클로덱스트린으로 생성시키는 산업적으로 가장 많이 응용되는 효소 중에 하나이다. 수용성 녹말을 기질로 하여 CLEC화한 Bacillus macerans $\alpha$-CGTase 효소를 극한의 반응 조건인 계면활성제나 유기 용매가 혼합된 반응조건에서 실험한 결과, 이들 조건이 싸이클로덱스트린의 생산을 증가시키는 영향을 초래하였고 특히, 계면활성제인 SDS와 $\beta$-OG는 전체 싸이클로덱스트린의 생성을 증가시켰고 이 중에서 SDS와 Lubrol PX는 알파싸이클로덱스트린의 생성의 특이성의 결과를, 반면에 Triton x-100과 Tween 80은 알파싸이클로덱스트린의 생성을 억제하는 결과를 보였다. 유기용매인 DMSO, formamide, MPD, ethylene glycol 또한 사이클로 덱스트린의 전체 수율과 특이성에 영향을 미치는 효력을 보였다.

• 농약과학회지
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• 제5권2호
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• pp.58-61
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• 2001

Fenoxaprop-ethyl R(+), S(-) 및 racemic mixture의 벼와 피에 대한 온실조건에서 제초활성 및 선택성과 aryloxyphenoxypropionate계열 제초제의 작용점으로 알려진 ACCase의 억제정도를 비교하였다. 온실에서의 벼와 피에 대한 식물체반응에서 R(+) 이성체가 가장 강한 생육저해를 보였고, S(-) 이성체에서 가장 약한 반응을 나타내어 fenoxaprop-ethyl R(+) 이성체가 활성형태임을 확인하였다. 온실에서 피에 대한 억제정도는 ACCase에 대한 in vitro 억제반응의 결과와 일치하여 fenoxaprop의 작용점은 효소 ACCase임을 알았다. 벼, 피간의 선택성 지수의 비교에서 온실실험의 결과 R(+)과 racemic mixture인 경우에는 각 각의 값이 0.6과 0.8로 비교적 낮았으나, S(-) 이성체의 경우에는 약 1.5로써 S(-) 이성체의 벼에 대한 안전성 폭이 R(+) 이성체보다 넓은 것으로 나타났다. 하지만, 이러한 경향이 in vitro수준에서는 이성체간 선택성지수의 차이는 인정되지 않았다. 따라서 작용점상에서 fenoxaprop-ethyl의 벼, 피간 근본적 선택성은 존재하지 않는 것으로 판단된다.

• Biomolecules & Therapeutics
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• 제16권4호
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• pp.336-342
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• 2008

The resveratrol analogue piceatannol (3,5,3',4'-tetrahydroxy-trans-stilbene) is a polyphenol present in grapes and wine and reported to have anti-carcinogenic activities. To investigate the mechanism of anticarcinogenic activities of piceatannol, the effects on CYP 1 enzymes were determined in Escherichia coli membranes coexpressing recombinant human CYP1A1, CYP1A2 or CYP1B1 with human NADPH-P450 reductase. Piceatannol showed a strong inhibition of CYP1A1 and CYP1B1 in a concentration-dependent manner, and $IC_{50}$ of human CYP1A1 and CYP1B1 was 5.8 ${\mu}M$ and 16.6 ${\mu}M$, respectively. However, piceatannol did not inhibit CYP1A2 activity in the concentration of up to 100 ${\mu}M$. Piceatannol exhibited 3-fold selectivity for CYP1B1 over CYP1A1. The mode of inhibition of piceatannol was non-competitive for CYP1A1 and CYP1B1. The result that piceatannol did not inhibit CYP1B1-mediated $\alpha$-naphthoflavone ($\alpha$-NF) metabolism suggests piceatannol may act as a non-competitive inhibitor as well. In human prostate carcinoma PC-3 cells, piceatannol induces apoptosis and prevents Aktmediated signal pathway. Taken together, abilities of piceatannol to induce apoptotic cell death as well as CYP1 enzyme inhibition make this compound a useful tool for cancer chemoprevention.