• Title/Summary/Keyword: ligands

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Identifiaction and Molecular Size of Zine-Binding Ligands in Pancreatic/Biliary Fluid of Rats

  • Kwun, In-Sook;Donald Oberleas
    • Preventive Nutrition and Food Science
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    • v.2 no.1
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    • pp.42-48
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    • 1997
  • the exocrine pancreatic secretion is an important factor in the maintenance of zinc homeostasis. The daily pancreatic secretion of zinc into the gastrointestinal tract may be two or more times the daily dietary zinc intake. The objective of this study was to examine the distribution of proteins and zinc in pancreatic/biliary fluid following intraperitoneal {TEX}${65}^Zn${/TEX} injection into dietary prepared Sprague-Dawly rats. Distribution of zinc-binding protein in Sephadex G-75 subfractions showed a peak corresponding to the high molecular weight protein standard(<66kDa) in the pancreatic/biliary fluid. Zinc also was associated with the 29~35kDa mole-cular weight proteins. These are similar in size with zinc-containing enzymes, carboxypeptidase A and car-boxypeptidase B. A more remarkable small molecular weight fraction eluted beyond the 6.5kDa standard pro-tein peak. These results show the presence of small molecular weight compound in pancreatic/biliary fluid associated with zinc . These small molecular weight compounds may serve as zinc-binding ligands for the secretion of enogenous zinc into the duodenum. These findings suggest that these lignads may dissociate zinc in the duodenum thus making it vulnerable to complexation with phytate in the upper gastrointestinal tract rendering the zinc unavailable for reabsorption.

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The Influence of Surface Modification of Gold Nanoparticles Supported on TiO2 in the Catalytic Activity of CO Oxidation

  • Park, Da-Hee;Reddy, A.S.;Eah, Sang-Kee;Park, Jeong-Young
    • Proceedings of the Korean Vacuum Society Conference
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    • 2011.08a
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    • pp.213-213
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    • 2011
  • Gold catalysts supported on TiO2 have shown a unique catalytic behavior on CO oxidation, depending on surface effects. Particle size has an influence on the surface activity. To make monodisperse Au nanoparticles, organic capping ligands, such as alkylthiols, were used by a "greener" synthesis method [1,2] and Au nanoparticles were deposited on TiO2. However, organic capping ligands must be removed for high catalytic activities by the Au nanoparticles without changing the Au size [3]. We used UV ozone treatment to decompose thiol ligands. The samples have been characterized by X-ray photoelectron spectroscopy to examine the surface modification by UV ozone treatment. We show the size distribution of the gold nanoparticles by light scattering analysis and transmission electron microscopy. Au/TiO2 have been prepared using the wetness impregnation method. The catalytic performance of CO oxidation over Au supported on TiO2 under oxidizing reaction conditions (40 Torr CO and 100 Torr O2) were tested. The results show that the catalytic activity depends on particle size and the time of UV ozone exposure, which suggests the role of sulfur bonding in determining the catalytic activity of Au/TiO2 catalysts.

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Systems Biological Approaches Reveal Non-additive Responses and Multiple Crosstalk Mechanisms between TLR and GPCR Signaling

  • Krishnan, Jayalakshmi;Choi, Sang-Dun
    • Genomics & Informatics
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    • v.10 no.3
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    • pp.153-166
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    • 2012
  • A variety of ligands differ in their capacity to bind the receptor, elicit gene expression, and modulate physiological responses. Such receptors include Toll-like receptors (TLRs), which recognize various patterns of pathogens and lead to primary innate immune activation against invaders, and G-protein coupled receptors (GPCRs), whose interaction with their cognate ligands activates heterotrimeric G proteins and regulates specific downstream effectors, including immuno-stimulating molecules. Once TLRs are activated, they lead to the expression of hundreds of genes together and bridge the arm of innate and adaptive immune responses. We characterized the gene expression profile of Toll-like receptor 4 (TLR4) in RAW 264.7 cells when it bound with its ligand, 2-keto-3-deoxyoctonate (KDO), the active part of lipopolysaccharide. In addition, to determine the network communications among the TLR, Janus kinase (JAK)/signal transducer and activator of transcription (STAT), and GPCR, we tested RAW 264.7 cells with KDO, interferon-${\beta}$, or cAMP analog 8-Br. The ligands were also administered as a pair of double and triple combinations.

Biopharmaceutical studies on copper(II) chelates of sulfanilamide derivatives (Sulfanilamide유도체의 동(II)착화합물에 대한 생물약제학적 연구)

  • 김재백
    • YAKHAK HOEJI
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    • v.15 no.2
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    • pp.41-52
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    • 1971
  • Cu(II) chelates of several sulfanilamide derivatives (Sulfa-Cu) were prepared and their effects on solubility, absorptivity in intestinal lumen, biding tendency with serum protein and erythrocytes, concentration in rabbit blood, and acetylation rate were studied in comparison with their free ligand forms. For solubility concerned, the partition coefficients of Sulfa-Cu are decreased as following order: Sulfadimethoxine Copper chelate (SDM-Cu), Sulfamethoxypyridazine Copper chelate (SD-Cu), Sulfamerazine Copper chelate (SM-Cu), Sulfaisoxazole Copper chelate (SIX-Cu). The partition coefficients of SDM-Cu and ST-Cu were much greater than those of ligands. this phenomenone acounts for the rapid absorption of SDM-Cu and ST-Cu in the rat small intestine (in situ). The Sulfa-Cu were absorbed at the intestinal lumen of a rat in the rate of first order and there was no difference between long acting sulfa drugs and their Cu0chelates in biological half lives. In binding experiments, sulfa-Cu binded with serum protein in lower ratio than their ligands except SIX-Cu. On other hand, acetylation rates of sulfa-Cu were higher than those of free sulfa drugs and the acetylation rate were higher than those of free sulfa drugs and powder. In a experiment on Sulfa-Cu concentration in rabbit blood, the half lives of SD-Cu, SIX-cu, ST-Cu, and SM-Cu were longer than those of their ligands. Above all, the half life of SD-Cu appeared to be approximately 3.5 times logner than that of corresponding ligand, SD. When absorption of sulfa drugs or sulfa-Cu at the small intestinal lumen of a rat and the concentration in rabbit blood after absorption were compared, it was found that there was not always conrrelated.

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The effective model of the human Acetyl-CoA Carboxylase inhibition by aromatic-structure inhibitors

  • Minh, Nguyen Truong Cong;Thanh, Bui Tho;Truong, Le Xuan;Suong, Nguyen Thi Bang;Thao, Le Thi Xuan
    • Journal of IKEEE
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    • v.21 no.3
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    • pp.309-319
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    • 2017
  • The research investigates the inhibition of fatty acid biosynthesis of the human Acetyl-CoA Carboxylase enzyme by the aromatic-structure inhibitors (also known as ligands) containing variables of substituents, contributing an important role in the treatment of fatty-acid metabolic syndrome expressed by the group of cardiovascular risk factors increasing the incidence of coronary heart disease and type-2 diabetes. The effective interoperability between ligand and enzyme is characterized by a 50% concentration of enzyme inhibitor ($IC_{50}$) which was determined by experiment, and the factor of geometry structure of the ligands which are modeled by quantum mechanical methods using HyperChem 8.0.10 and Gaussian 09W softwares, combining with the calculation of quantum chemical and chemico-physical structural parameters using HyperChem 8.0.10 and Padel Descriptor 2.21 softwares. The result data are processed with the combination of classical statistical methods and modern bioinformatics methods using the statistical softwares of Department of Pharmaceutical Technology - Jadavpur University - India and R v3.3.1 software in order to accomplish a model of the quantitative structure - activity relationship between aromatic-structure ligands inhibiting fatty acid biosynthesis of the human Acetyl-CoA Carboxylase.

Bulk Coordination Polymerization of Dicyclopentadiene (DCPD) by Pd Complexes Containing β-Ketoiminate or β-Diketiminate Ligands

  • Lee, Eung Jun;Kim, Ho Sup;Lee, Byoung Ki;Hwang, Woon Sung;Sung, Ik Kyoung;Lee, Ik Mo
    • Bulletin of the Korean Chemical Society
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    • v.33 no.12
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    • pp.4131-4136
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    • 2012
  • Several palladium complexes containing ${\beta}$-ketoiminate and ${\beta}$-diketiminate ligands successfully produced poly(DCPD) possibly via vinyl addition. It was found that catalysts with ${\beta}$-diketiminate ligands containing bulkier aryl substituents showed the highest activity in the presence of MAO as a cocatalyst. Purity of DCPD is quite essential for the higher activity and small amount of organic solvent such as $CH_2Cl_2$ and toluene is required to reduce the viscosity of the reactant mixture for the higher activity. $^1H$ NMR spectra of produced polymers with N,N-dimethylanilinium tetra(pentafluorophenyl)borate (N,N-DAPFAr"$_4$) show that 5,6-double bond of DCPD is removed with 2,3-double bond remaining. Produced poly(DCPD) with MAO cocatalyst is quite rigid and insoluble in common organic solvents but rather brittle.

Determination of Uranyl Nitrate with Several Ligands by Spectrophotometry

  • Showkat, Ali Md.;Zhang, Yu-Ping;Kim, Min Seok;Kim, Sang-Ho;Choi, Seong-Ho;Lee, Kwang-Pill
    • Analytical Science and Technology
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    • v.17 no.1
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    • pp.23-28
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    • 2004
  • Trace amount of uranyl (II) has been determined spectrophotometrically by measuring the optical density of the light blue yellowish coloured solutions formed by reaction between the metal ion and nicotinohydroxamic acid (NHx) in presence of different secondary ligands in strong isoamyl alcohol alkaline medium. The absorption maxima for both aqueous and extracted systems measured at their respective optimum pH were found to be 360 and 559 nm (DETA), 375 and 358 nm (EDA), 369 and 362 nm (piperidine), 354 and 341 nm (pyridine) and 363 and 336 nm (3 piperidine), 354 and 341 nm (pyridine) and 363 and 336 nm (3 - picoline), respectively at which Beer's law was obeyed. Effect of pH, reagent concentration, order of addition of reagent, time, temperature and solvent media on the absorption spectra have also been studied. Among the different systems studied, the shortest concentration range of uranyl(II) adhering to Beer's Law was 2.4 - 10.5 ppm observed for $UO_2(II)$ - NHx - DETA system in aqueous medium and also for iso amyl alcohol(IAA) extracted $UO_2$ - NHx - pyridine system was 2.4 - 7.8.

EphB/ephrinB Signaling in Cell Adhesion and Migration

  • Park, Inji;Lee, Hyun-Shik
    • Molecules and Cells
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    • v.38 no.1
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    • pp.14-19
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    • 2015
  • Eph receptors and their ligands, ephrins, represent the largest group of the receptor tyrosine kinase (RTK) family, and they mediate numerous developmental processes in a variety of organisms. Ephrins are membrane-bound proteins that are mainly divided into two classes: A class ephrins, which are linked to the membrane by a glycosylphosphatidylinositol (GPI) linkage, and B class ephrins, which are transmembrane ligands. Based on their domain structures and affinities for ligand binding, the Eph receptors are also divided into two groups. Trans-dimerization of Eph receptors with their membrane-tethered ligands regulates cell-cell interactions and initiates bidirectional signaling pathways. These pathways are intimately involved in regulating cytoskeleton dynamics, cell migration, and alterations in cellular dynamics and shapes. The EphBs and ephrinBs are specifically localized and modified to promote higher-order clustering and initiate of bidirectional signaling. In this review, we present an in-depth overview of the structure, mechanisms, cell signaling, and functions of EphB/ephrinB in cell adhesion and migration.

Calculation of the Dipole Moments for the Coordination Compounds with Organic Ligands such as $(C_2H_5)_2SO,\;(C_6H_5)_2SO,\;(C_6H_5)_2SeO,\;(C_6H_5)_3AsO,\;(C_6H_5)_3PBCl_3,\;and\;(C_2H_5)_2OZrCl_4$

  • Ahn, Sang-Woon;Kim, Hyung-Doo;Park, Eui-Suh
    • Bulletin of the Korean Chemical Society
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    • v.7 no.2
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    • pp.129-136
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    • 1986
  • The dipole moments for some coordination compounds with organic ligands have been calculated adopting the molecuar orbitals obtained from EHT calculation with modified technique. Adopting the molecular orbitals with the modified technique, the calculated dipole moments for all the coordination compounds with organic ligands give closer agreements with experimental values than those using the molecular orbitals obtained from EHT calculation. The calculated dipole moments suggest that $(C_2H_5)_2SO,\;(C_6H_5)_2SO,\;and\;(C_6H_5)_2SeO$ may have a trigonal planar structure and $(C_6H_5)_3AsO,\;and\;(C_6H_5)_3PBCl_3$ a square planar structure and $(C_2H_5)_2OZrCl_4$ may be distorted markedly. This work may also indicate that the modified technique is superior to the EHT calculation as far as the dipole moment calculation is concerned.

Influence of Coating Ligands onf Enzyme-linked Immunosorbent Assay of Toluene

  • Kim, So Yeong;Lee, Nam Taek;Choe, Myeong Ja
    • Bulletin of the Korean Chemical Society
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    • v.22 no.9
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    • pp.953-957
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    • 2001
  • The specificity of conjugation site for coating ligands was investigated using toluene-bovine serum albumin (BSA) conjugates in which BSA was conjugated at the position of o-, m-, and ${\rho}-toluic$ acid. Toluene-BSA conjugated at ${\rho}-position$ showed a binding activity of about 89-95%, whereas, those conjugated at o- and m-position of toluene exhibited a binding activity of 5 and 11%, respectively. On the basis of the above result, coating ligands with various proteins (OVA, BSA, KLH) were compared by conjugating with $\rho-toluic$ acid, and toluene-KLH was considered as the best coating ligand for this ELISA. Indirect competitive ELISA method was developed using anti-toluene antibody and $\rho-position$ conjugated toluene-KLH. The dose-response curve constructed after kinetic and optimization studies showed a 1${\times}$10-4 - 1${\times}$102 mM detectable response range with 0.1 ${\mu}M$ detectability. In specificity test of the antibody, the binding capabilities of aromatic compounds substituted with nitro-, alkyl-, chloro-, and hydroxyl group were larger rather than those of aromatic compounds (benzene, toluene and xylene) themselves. Also, tests with soil and water samples that had been spiked with toluene resulted in 102.7-113.7% recovery.