• Molecules and Cells
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• 제27권6호
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• pp.651-656
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• 2009

The formation of ${\beta}$-amyloid peptide ($A{\beta}$) is initiated from cleavage of amyloid precursor protein (APP) by a family of protease, ${\alpha}$-, ${\beta}$-, and ${\gamma}$-secretase. Sub W, a substrate peptide, consists of 10 amino acids, which are adjacent to the ${\beta}$-cleavage site of wild-type APP, and Sub M is Swedish mutant with double mutations on the left side of the ${\beta}$-cleavage site of APP. Sub W is a normal product of the metabolism of APP in the secretary pathway. Sub M is known to increase the efficiency of ${\beta}$-secretase activity, resulting in a more specific binding model compared to Sub W. Three-dimensional structures of Sub W and Sub M were studied by CD and NMR spectroscopy in water solution. On the basis of these structures, interaction models of ${\beta}$-secretase and substrate peptides were determined by molecular dynamics simulation. Four hydrogen bonds and one water-mediated interaction were formed in the docking models. In particular, the hydrogen bonding network of Sub M-BACE formed spread over the broad region of the active site of ${\beta}$-secretase (P5-P3'), and the side chain of P2- Asn formed a hydrogen bond specifically with the side chain of Arg235. These are more favorable to the cleavage of Sub M by ${\beta}$-secretase than Sub W. The two substrate peptides showed different tendency to bind to ${\beta}$-secretase and this information may useful for drug development to treat and prevent Alzheimer's disease.

• 한국토양환경학회지
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• 제4권3호
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• pp.17-24
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• 1999

토양오염 디이젤 제거에 대한 토양 세척기술의 적용을 위해 디이젤 제거효과가 좋은 비이온 계면활성제를 선택하기 위한 조건 중 소수성 사슬구조의 영향을 고찰하였다. 비이온 계면활성제는 CMC값이 낮고, 생분해성이 좋으며, 유기 오염물질에 대한 용해 능력이 커서 디이젤과 같은 NAPL류 제거에 효과적으로 사용될 수 있다. 비이온계 계면활성제 구조 내 소수성 탄화수소 사슬의 길이와 불포화결합의 존재는 흡착과 디이젤 제거에 영향을 미치며, 비이온계 계면활성제의 kaolin토양흡착과 디이젤 제거는 서로 밀접한 관계를 가지고 있다. 친수성기의 구조가 서로 동일한 계면활성제 중에서 소수성 탄화수소 사슬길이가 12개로 비교적 짧고 HLB값이 클 때 상대적으로 낮은 흡착평형농도와 높은 디이젤 제거효율을 나타냈다. 소수성 사슬 내에 불포화 탄화수소가 존재할 때 낮은 흡착평형농도와 높은 디이젤 제거 효율을 나타냈다. 농도에 따른 제거경향은 흡착이 평형에 도달한 후에 최대의 제거 효율을 나타냈으며 그 이상의 농도에서는 오히려 제거효율이 감소하는 현상이 나타났다.

• BMB Reports
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• 제30권5호
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• pp.370-377
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• 1997

A novel assay method is described for rapid quantitation of reaction rate of sterol ${\Delta}^7$-reductase (${\Delta}^7$-SR) which catalyzes reduction of the ${\Delta}^7$-double bond of sterols. Of six different organ tissues-liver, small intestine, brain, lung, kidney, and testis-. ${\Delta}^7$-SR activity was detected only in liver (2.30 nmol/min/mg protein) and testis (0.11 nmol/min/mg protein). Using a newly developed method which employs diet-induced enzyme proteins and ergosterol as substrate, we assessed both kinetics ($K_m=210\;{\mu}M$, $V_{max}=1.93\;nmol/min/mg$) and inhibition of the rat hepatic ${\Delta}^7$-SR against well-studied cholesterol lowering agents such as triparanol ($IC_{50}=16\;{\mu}M$). 3-$\beta$-[2-(diethylamino)ethoxy]androst-5-en-17-one (U18666A) ($IC_{50}=5.2\;{\mu}M$), and trans-1.4-bis(2-chlorobenzylaminomethyl)cyclohexane dihydrochloride (AY-9944) ($IC_{50}=0.25\;{\mu}M$). Of the three well-known AY-9944-sensitive cholesterogenic enzymes (i.e., ${\Delta}^7$-SR, sterol ${\Delta}^8$-isomerase, and sterol ${\Delta}^14$-reductase). ${\Delta}^7$-SR was found to be the most sensitive enzyme with a noncompetitive inhibition of this compound ($K_i=0.109\;{\mu}M$). Substrate specificity studies of the microsomal ${\Delta}^7$-SR indicate that the relative reaction rate for 7-dehydrocholesterol and ergosterol are 5.6-fold and 1.6-fold higher than that for lathosterol. ${\Delta}^7$-SR activity was also modulated by feeding rats a diet supplemented with 0.5% ergosterol (>2.6-fold) in addition to 5.0% cholestyramine plus 0.1% lovastatin ($\simeq$5.0-fold). Finally, microsomal ${\Delta}^7$-SR was solubilized by 1.5% 3-[3-(cholamidopropyl)-dimethylammonio]-1-propanesulfonate (CHAPS) and enriched on PEG (0~10%) precipitation, which should be suitable for further purification of the enzyme.

• Journal of Photoscience
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• 제10권1호
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• pp.9-20
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• 2003

Recent studies on the photoreactivity of l,4-unsaturated systems have changed some ideas that were firmly established in this area of research for many years. Thus, we have described the first examples of 2-aza-di-$\pi$-methane (2-ADPM) rearrangements promoted by triplet-sensitization and by single electron transfer (SET) using electron-acceptor sensitizers. These reactions afford N-vinylaziridine and cyclopropylimine photoproducts in the first examples of di-$\pi$-methane processes that yield three-membered ring heterocycles. l-Aza-1,4-dienes also undergo SET-promoted l-aza-di-$\pi$-methane (l-ADPM) rearrangements via radical-cation intermediates using electron acceptor sensitizers. In some cases, alternative cyclizations yielding different carbocycles and heterocycles have been observed. The l-ADPM and di-$\pi$-methane (DPM) reactions also occur via radical-anion intermediates on irradiation using electron donor sensitizers. On the other hand, the photoreactivity reported for $\beta$,${\gamma}$-unsaturated aldehydes for many years was decarbonylation to the corresponding alkenes. However, our studies demonstrate that these compounds undergo the oxa-di-$\pi$-methane (ODPM) rearrangement with high chemical and quantum efficiency. A comparison of the photochemical reactivity of $\beta$,${\gamma}$-unsaturated aldehydes and corresponding methyl ketones has shown that the ketones do not undergo the ODPM rearrangement while the corresponding aldehydes are reactive by this pathway. Monosubstituted $\beta$,${\gamma}$-unsaturated aldehydes at C-2 undergo the ODPM rearrangement yielding the corresponding cyclopropane carbaldehydes diastereoselectively. Finally, we have described the first examples of reactions, similar to the well know Norrish Type I process, which take place in the triplet excited state of $\beta$,${\gamma}$-unsaturated carbonyl compounds by excitation of the C-C double bond instead of the carbonyl group.

• Journal of Pharmaceutical Investigation
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• 제36권3호
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• pp.169-174
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• 2006

The aim of this work was to prepare tenoxicam-ethanolamine salt with improved physicochemical properties for transdermal application. Tenoxicam-ethanolamine salt was prepared in methylene chloride and its physicochemical properties were investigated by DSC and FT-lR. The broad peak of tenoxicam around 3600-3200 $cm^-1$ was shifted to lower wavenumber and more broadened. The characteristic endothermic melting peak of tenoxicam appeared at $223^{\circ}C$. The melting peak of tenoxicam-ethanolamine salt was shifted to $159^{\circ}C$. In contrast to relatively small difference in the partition coefficients of tenoxicam and the tenoxicam-ethanolamine salt, large difference in aqueous solubility was observed. $Crovol^{\circledR}$ PK4O (PEG-12 palm kernel glycerides) provided the highest skin flux for both compounds. The order of the enhancing effect of the various vehicles tested was similar for tenoxicam and tenoxicam-ethanolamine salt, which indicated that their enhancing mechanism for tenoxicam and tenoxicam-ethanolamine salt is similar. Tenoxicam-ethanolamine salt had a higher skin flux than tenoxicam by 1.2- to 31.7-fold, depending on the vehicles used. It is suggested that the vehicles with medium HLB value, 1 double bond, and lower ethylene oxide chain length have a better ability to modify the permeability of the stratum corneum and to promote the effective penetration of tenoxicam and tenoxicam-ethanolamine salt.

• 한국미생물·생명공학회지
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• 제46권2호
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• pp.145-153
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• 2018

Among the carotenoid biosynthesis genes, crtI gene encodes the phytoene desaturase (CrtI) enzyme, and phytoene desaturase convert phytoene to lycopene. Phytoene desaturase is involved in the dehydrogenation reaction, in which four single bonds in the phytoene are introduced into a double bond, eliminating eight hydrogen atoms in the process. Phytoene desaturase is one of the key regulating enzyme in carotenoid biosynthetic pathway of various carotenoid biosynthetic organisms. The crtI gene in genomic DNA of Paracoccus haeundaensis was amplified and cloned into a T-vector to analyze the nucleotide sequence. As a result, the crtI gene coding for phytoene desaturase from P. haeundaensis consists of 1,503 base pairs encoding 501 amino acids residues. An expression plasmid containing the crtI gene was constructed, and Escherichia coli cells containing this plasmid produced the recombinant protein of approximately 55 kDa, equivalent to the molecular weight of phytoene desaturase. The expressed protein in cell lysate showed enzymatic activity similar to phytoene desaturase. Phytoene and lycopene were analyzed by HPLC and measured at wavelength of 280 nm and 470 nm, respectively. The $K_m$ values for phytoene and NADPH were $11.1{\mu}M$ and $129.3{\mu}M$, respectively.

• Elastomers and Composites
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• 제34권3호
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• pp.229-238
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• 1999

본 연구에서는 제3의 성분으로 벤젠 술폰산계열 반응성 화합물과 ENB 및 DCPD를 사용하여 비diene계 고분자인 EVA를 특수 화학적 처리에 의하여 EVA의 주쇄에 불포화기 즉, 이중결합을 도입시켰다. 또한 이중결합도입 EVA와 diene계 범용합성고무인 CR, SBR과의 블렌드를 통하여 황가 황체를 제조하여 가황체들의 물리적 특성을 비교 검토하였다. 검토결과 원래의 EVA가 갖고 있는 green strength, 사출 압출 성형성, 접착성, 점착성, 치수안정성, 오존저항성 등의 장점은 그대로 살리면서도 황가황이 가능하여 열가소성의 EVA가 갖는 사용온도의 한계 문제와 기계적 특성 즉, 경도, 인장강도, 인장 응력, 신장율 등온 향상시켰다. 비diene계 고분자와 diene계 고분자의 블렌드에 있어서 개질에 대한 연구가 더 수행되어진다면 합성고무에서 나타나는 부족한 가공성, 내산화 안정성, 접착성 등을 크게 향상시킬 수 있을 것이며 아울러 EVA의 융해유동성을 이용한 고무제품 가공공정의 연속화가 가능하게 될 것이다.

• 폴리머
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• 제34권5호
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• pp.391-397
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• 2010

폴리아믹산(PAA)은 가교가 가능한 2중 결합을 갖는 bicyclo(2,2,2)oct-7-ene-2,3,5,6-tetracarboxy-licdianhydride(BTDA)와 bis[4-(3-aminophenoxy)phenyl] sulfone(BAPS)을 N,N-dimethylacetamide(DMAc) 용매에서 반응하여 얻어졌으며, 폴리이미드(PI) 필름은 PAA를 캐스팅하여 각각 다른 반응 온도에서 열처리를 통해 얻었다. 가교 온도를 $250{\sim}350^{\circ}C$까지 증가하여 얻은 가교된 PI의 열적-기계적 성질, 가교도, 광학적 특성을 열처리 온도에 따라 조사하였다. 열적-기계적 성질은 $350^{\circ}C$에서 열처리되었을 때 최대 값을 나타냈으며, 광학적 특성은 $250^{\circ}C$에서 열처리된 필름이 가장 우수한 광학특성을 보였다. $250{\sim}350^{\circ}C$까지 열처리에 따른 가교도는 NMR 상에서 85~93%를 나타냈다.

• 대한화학회지
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• 제18권3호
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• pp.180-188
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• 1974

Layer silicate 에 지지된 陽이온상에서의 일어난 acetaldehyde, acrolein, 그리고 crotonaldehyde의 吸着機構에 對하여 IR과 X-ray로서 硏究하였다. $1720∼1580㎝^{-1}$의 범위에서 일어난 4個의 특성적인 吸捉 band를 分析한 結果 $130㎝^{-1}$程度로 shift한 carbonyl band 는 >C=O${\cdots}$M형 complex 形成에 基因하는 것이었고, acetaldehyde는 $1722㎝^{-1}$에서, 다른 알데히드는 $1690㎝^{-1}$에서 sharp하게 나타난 carbonyl band는 >C=O와 surface -O-H와의 interaction에서 일어난 것이었다. 그리고 1710∼1660㎝-1에서 나타난 broad한 band는 >C=O와 陽이온 -O-H와의 사이에 일어난 水素結合에 依한 것이었다. 그리고 $1640∼1660㎝^{-1}$사이에 나타난 弱한 band는 carbonyl group 의 强한 吸着에 依하여 誤起된 >C=C< 二重結合에 依한 것이었다. 이 사실들은 X-ray 廻折에 依하여 다시 確認하였다.

• 대한화학회지
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• 제26권3호
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• pp.172-178
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• 1982

4',5'-디히드로소랄렌(DHP)을 합성하여 상온 및 77K에서 이 화합물의 형광 양자수율은 0.08, 인광양자수율은 0.013, 형광수명은 0.95ns, 인광수명은 0.039s 임을 알았다. 이 결과로부터 형광수명은 5,7-디메톡시쿠마린보다 작은반면 소랄렌보다 크고 반면 인광수명은 DMC 보다 크고 소랄렌보다 작음을 알았다. 소랄렌 유도체들의 광독성을 분자적 차원에서 규명하고 DNA에의 광부가 반응을 알아내기 위하여 DHP와 TME의 광부가 반응을 연구하였다. 주 생성물은 TLC로 분석하고 Preparative TLC와 용매추출로 분리해냈다. 분리된 생성물의 구조는 질량분석기, UV, IR, NMR 그리고 원소분석결과에 의해 DHP와 TME외 광고리화첨가반응에 의한 생성물 임을 알았다. DHP는 형광의 자체소광 효과를 볼 수 없으며 TME, 에틸푸마레이트, 푸마로니트릴에 의해 형광이 효과적으로 소광된다. 광부가 반응의 양자수율과 소광실험에서 DHP의 광첨가반응은 단일상태와 삼중상태에서 다 일어나는 것으로 추측된다.