• 제목/요약/키워드: Binding state

검색결과 481건 처리시간 0.027초

Behavior in Solution and Mixing Ratio-Dependent Binding Modes of Carcinogenic Benzo[a]pyrene-7,8-dione to Calf Thymus DNA

  • Jin, Biao;Han, Sung Wook;Lee, Dong Jin
    • Bulletin of the Korean Chemical Society
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    • 제35권10호
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    • pp.3015-3020
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    • 2014
  • The behavior of benzo[a]pyrene-7,8-dione (BPQ) in aqueous solution and its interaction with native DNA was investigated using conventional absorption and linear dichroism (LD) spectroscopy. The appearance of a broad absorption maximum at long wavelengths and its proportional relationship to solvent polarizability suggested that BPQ adopts a aggregated state for all solutions examined. Disappearance of this absorption band at higher temperatures in aqueous solution also supported BPQ aggregation. When associated with DNA absorption spectral properties were essentially the same as that in aqueous solution. However, two isosbestic wavelengths were found in the concentration-dependent absorption spectrum of the BPQ-DNA complex, suggesting the presence of at least two or more DNA-bound BPQ species. Both species produced $LD^r$ spectra whose magnitude in BPQ absorption region is larger or comparable to that in the DNA absorption region, suggesting that the molecular BPQ plane is near perpendicular relative to the local DNA helical axis. Therefore, BPQ molecules are aligned along the DNA stem in both DNA-aggregated BPQ species.

Comparison of Photocyclization Reactions of Fluoro- vs Nonfluoro-Substituted Polymethyleneoxy Donor Linked Phthalimides

  • Park, Hea Jung;Ryu, Young Ju;Kim, Kyung Mok;Yoon, Ung Chan;Kim, Eunae;Sohn, Youngku;Cho, Dae Won;Mariano, Patrick S.
    • Bulletin of the Korean Chemical Society
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    • 제34권4호
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    • pp.1108-1114
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    • 2013
  • Photochemical reactions of fluoro- vs. nonfluoro-substituted polymethylenoxy chain linked phthalimide were carried out to explore how electronegative fluorine atoms inside the donor chain influence photocyclization reaction efficiencies and to briefly determine the alkali metal binding properties of the photoproducts. The results of this study show that the fluorine-substituted donor chain linked phthalimide undergoes inefficient photocyclization via single electron transfer (SET)-induced excited state pathways to generate 14-membered cyclic amidol compared to nonfluoro-analog due to low electron donor ability of the terminal oxygen donor site. These results show that photoinduced intramolecular SET processes arising from ${\alpha}$-silyl ether electron donors to phthalimides are largely dependent on the kinds of substituents inside donor chain. Finally, a preliminary study with the cyclic amidols generated in this effort showed that they have weak alkali metal cation binding properties regardless of absence/presence of fluoro-substituents.

결정질AZO 박막과 비정질IGZO 박막의 결정구조와 결합에너지와의 상관성 (A Study on the Chemical Properties of AZO with Crystal Structure and IGZO of Amorphous Structure Due to the Annealing Temperature)

  • 소영호;송정호;서동명;오데레사
    • 산업진흥연구
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    • 제1권1호
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    • pp.1-6
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    • 2016
  • 산화물반도체의 결정질특성과 비정질특성을 이해하기 이하여 AZO 박막과 IGZO 박막을 증착하고 열처리하여 물리적 화학적인 특성을 비교하였다. AZO 박막은 열처리온도가 올라갈수록 결정성이 높아졌으나 IGZO 박막은 열처리온도가 높을수록 비정질특성이 우수하였다. AZO 박막은 열처리에 따라서 PL, XPS 분석에서 화학적 이동이 나타났으나 IGZO 박막은 화학적 이동이 나타나지 않았다. AZO의 O 1s 결합 에너지는 531.5 eV였으며, IGZO 박막은 530 eV으로 낮았다.

Expression and purification of human mPGES-1 in E. coli and identification of inhibitory compounds from a drug-library

  • Kim, Woo-Il;Choi, Kyung-A;Do , Hyun-Soo;Yu, Yeon-Gyu
    • BMB Reports
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    • 제41권11호
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    • pp.808-813
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    • 2008
  • Human microsomal prostaglandin E synthase-1 (mPGES-1) is a membrane associated protein that catalyzes the conversion of prostaglandin $H_2$ ($PGH_2$) into prostaglandin $E_2$ ($PGE_2$). In this study, the expression of human mPGES-1 in E. coli was significantly enhanced by modifying the utility of specific codons and the recombinant mPGES-1 was efficiently purified to homogeneity. The $K_m$ and $V_{max}$ of the purified enzyme were determined and the trimeric state characterized by chemical cross-linking with glutaraldehyde. The purified mPGES-1 was used for the screening of a chemical library of bioactive or drug compounds to identify novel inhibitors, and oxacillin and dyphylline were identified as moderately inhibiting mPGES-1 with $I_{C50}$ values of 100 and 200 ${\mu}M$, respectively. As these compounds competitively inhibited the catalysis of $PGH_2$, their binding sites appeared to be located near the $PGH_2$ binding pocket.

The pH Studies of Recombinant Acetohydroxy Acid Synthase from Tobacco

  • Choi, Jung-Do;Kim, Bok-Hwan;Yoon, Moon-Young
    • Bulletin of the Korean Chemical Society
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    • 제24권5호
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    • pp.627-632
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    • 2003
  • The pH dependence of the kinetic parameters of recombinant acetohydroxy acid synthase catalyzed reaction was determined in order to obtain information about the chemical mechanism, particularly acid-base chemistry. The maximum velocity and V/K for pyruvate were bell-shaped with estimated pK values of 6.5-6.7 and 8.6-8.9, respectively. The maximum velocity and V/K for 2-ketobutyrate were also bell-shaped with estimated pK values of 6.6-7.0 and 8.4-8.6. The pH dependence of 1/Ki for 3-bromopyruvate, a competitive inhibitor of pyruvate, was also bell-shaped, giving pK values almost identical with those obtained for pyruvate. Since the same pK values were observed in the $pK_{i 3-bromopyruvate}$, V/K pH profiles and $V_{max}$ profiles, both enzyme groups must be in their optimum protonation state for efficient binding of reactants. These results reflect that two enzyme groups are necessary for binding of substrate and/or catalysis.

Synthesis of Decapeptide of L-Aspartic Acid and Benzyl-L-Aspartic Acid by Solid Phase Peptide Synthesis

  • Yoo, Bong-K.;Jalil Miah, M.A.;Lee, Eung-Seok;Han, Kun
    • Archives of Pharmacal Research
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    • 제28권7호
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    • pp.756-760
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    • 2005
  • Polyene macrolide amphotericin B (AmB) is the drug of choice for the treatment of disseminated fungal infections. However, because of its pronounced side effects, the drug has limited applicability. There are few interesting reports, which state that co-administration of the drug with homo-peptide of polyaspartic acid reduces the side effects of the drug. In our present study, an approach has been made to systematically synthesize low molecular weight heteropeptides consisting of L-aspartic acid and its derivative. It was hypothesized that such heteropeptides will reduce the toxic side effects of the drug by facile hydrophobic binding between the polymer and the drug. We have employed the strategy of solid phase peptide synthesis (SPPS) to synthesize low molecular weight hetero-peptides by using L-aspartic acid and benzyl-L-aspartic acid to induce the hydrophobic binding between the peptide and the drug. In future, the proposed methodology can be employed to tailor other polypeptides substituted with benzyl groups to reduce the nephrotoxicity of AmB.

기능적 전기자극에 의한 근육피로의 특성을 표현하는 근육 모델 (Musculotendon Model to Represent Characteristics of Muscle Fatigue due to Functional Electrical Stimulation)

  • 임종광;남문현
    • 대한전기학회논문지:전력기술부문A
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    • 제48권8호
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    • pp.1046-1053
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    • 1999
  • The musculotendon model is presented to show the declines in muscle force and shortening velocity during muscle fatigue due to the repeated functional electrical stimulation (FES). It consists of the nonlinear activation and contraction dynamics including physiological concepts of muscle fatigue. The activation dynamics represents $Ca^{2+}$ binding and unbinding mechanism with troponins of cross-bridges in sarcoplasm. It has the constant binding rate or activation time constant and two step nonlinear unbinding rate or inactivation time constant. The contraction dynamics is the modified Hill type model to represent muscle force - length and muscle force - velocity relations. A muscle fatigue profile as a function of the intracellular acidification, pH is applied into the contraction dynamics to represent the force decline. The computer simulation shows that muscle force and shortening velocity decline in stimulation time. And we validate the model. The model can predicts the proper muscle force without changing its parameters even when existing the estimation errors of the optimal fiber length. The change in the estimate of the optimal fiber length has an effect only on muscle time constant in transient period not on the tetanic force in the steady-state and relaxation periods.

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Dioxygen Binding to the Singly Alkoxo-Bridged Diferrous Complex: Properties of [$Fe^{Ⅱ}_2$(N-Et-HPTB)$Cl_2$]$BPh_4$

  • 김은석;이강봉;Jang, Ho G.
    • Bulletin of the Korean Chemical Society
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    • 제17권12호
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    • pp.1127-1131
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    • 1996
  • [FeⅡ2(N-Et-HPTB)Cl2]BPh4(1), where N-Et-HPTB is the anion of N,N,N',N'-tetrakis(N-ethyl-2-benzimidazolylmethyl)-2-hydroxy-l,3-diaminopropane, has been synthesized to model dioxygen binding to the diferrous centers of proteins. 1 has a singly bridged structure with a μ-alkoxo of N-Et-HPTB and contains two five-coordinate iron(Ⅱ) centers with two chloride ligands as exogenous ligands. 1 exhibits an electronic spectrum with a λmax at 336 nm in acetone. 1 in acetone exhibits no EPR signal at 4 K, indicating diiron(Ⅱ) centers are antiferromagnetically coupled. Exposure of acetone solution of 1 to O2 at -90 ℃ affords an intense blue color intermediate showing a broad band at 586 nm. This absorption maximum of the dioxygen adduct(1/O2) was found in the same region of μ-l,2-peroxo diiron(Ⅲ) intermediates in the related complexes with pendant pyridine or benzimidazole ligand systems. However, this blue intermediate exhibits EPR signals at g = 1.93, 1.76, and 1.59 at 4 K. These g values are characteristic of S = 1/2 system derived from an antiferromagnetically coupled high-spin Fe(Ⅱ)Fe(Ⅲ) units. 1 is the unique example of a (μ-alkoxo)diferrous complex which can bind dioxygen and form a metastable mixed-valence intermediate. At ambient temperature, most of 1/O2 intermediate decays to form a diamagnetic species. It suggests that the dacay reaction of the intermediate might be bimolecular, implying the formation of mixed-valence tetranuclear species in transition state.

Characterization of the Nanog 5'-flanking Region in Bovine

  • Choi, Don-Ho;Kim, Duk-Jung;Song, Ki-Duk;Park, Hwan-Hee;Ko, Tae Hyun;Pyao, Yuliya;Chung, Ku-Min;Cha, Seok Ho;Sin, Young-Su;Kim, Nam-Hyung;Lee, Woon-Kyu
    • Asian-Australasian Journal of Animal Sciences
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    • 제29권10호
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    • pp.1383-1391
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    • 2016
  • Bovine embryonic stem cells have potential for use in research, such as transgenic cattle generation and the study of developmental gene regulation. The Nanog may play a critical role in maintenance of the undifferentiated state of embryonic stem cells in the bovine, as in murine and human. Nevertheless, efforts to study the bovine Nanog for pluripotency-maintaining factors have been insufficient. In this study, in order to understand the mechanisms of transcriptional regulation of the bovine Nanog, the 5'-flanking region of the Nanog was isolated from ear cells of Hanwoo. Results of transient transfection using a luciferase reporter gene under the control of serially deleted 5'-flanking sequences revealed that the -134 to -19 region contained the positive regulatory sequences for the transcription of the bovine Nanog. Results from mutagenesis studies demonstrated that the Sp1-binding site that is located in the proximal promoter region plays an important role in transcriptional activity of the bovine Nanog promoter. The electrophoretic mobility shift assay with the Sp1 specific antibody confirmed the specific binding of Sp1 transcription factor to this site. In addition, significant inhibition of Nanog promoter activity by the Sp1 mutant was observed in murine embryonic stem cells. Furthermore, chromatin-immunoprecipitation assay with the Sp1 specific antibody confirmed the specific binding of Sp1 transcription factor to this site. These results suggest that Sp1 is an essential regulatory factor for bovine Nanog transcriptional activity.

Separation of Phosvitin from Egg Yolk without Using Organic Solvents

  • Jung, Samooel;Ahn, Dong Uk;Nam, Ki Chang;Kim, Hyun Joo;Jo, Cheorun
    • Asian-Australasian Journal of Animal Sciences
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    • 제26권11호
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    • pp.1622-1629
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    • 2013
  • The objective of this study was to develop a new method to separate phosvitin from egg yolk without using organic solvents. Phosvitin was extracted from yolk granules using 10% NaCl or 10% $(NH_4)_2SO_4$ (final concentration) and then treated with heat to precipitate the lipoproteins from the extracted solution. The optimal pH for the phosvitin extraction from yolk granules was determined, and the iron-binding ability of the extracted phosvitin (final product) was tested. Adding 10% $(NH_4)_2SO_4$ disrupted the granules, and the subsequent thermal treatment at $90^{\circ}C$ for 1 h precipitated low density and high density lipoproteins, which enabled separation of phosvitin by centrifugation. The phosvitin concentration in the extract was significantly higher when the pH of the solution was adjusted to pH ${\geq}9$. The purity and recovery rate of phosvitin at the end of the separation process were approximately 78% and 56%, respectively. The separated phosvitin was confirmed to have ferrous and ferric iron binding ability. The advantages of this new method compared with the traditional methods include no organic solvents and high-priced equipment are needed for the separation. Also, this method is more environment and consumer friendly than that of the traditional methods.