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511.
Effects of the Surface Densities of Glycoclusters on the Determination of Their IC50 and Kd Value Determination by Using a Microarray 下载免费PDF全文
Lucie Dupin Francesca Zuttion Dr. Thomas Géhin Albert Meyer Prof. Dr. Magali Phaner‐Goutorbe Dr. Jean‐Jacques Vasseur Dr. Eliane Souteyrand Dr. François Morvan Dr. Yann Chevolot 《Chembiochem : a European journal of chemical biology》2015,16(16):2329-2336
Pseudomonas aeruginosa (PA) is an opportunistic bacterium involved in 10–30 % of nosocomial diseases. It causes severe lung injury to cystic fibrosis patients, often leading to patient death. PA strains are multidrug resistant, thus making the design of new therapeutics a challenge for public health. One promising therapeutic option is to design glycoclusters that target the virulence factor of PA. LecA is a galactose‐specific lectin that might be involved in adhesion and biofilm formation by PA. The DNA‐directed immobilization (DDI) microarray is a powerful tool for screening and understanding of structure–activity relationships between glycoclusters and lectins. High‐throughput and multiplexed analysis of lectin–glycocluster interactions on a DDI microarray allows measurement of IC50 and dissociation constant (Kd) values with minute amounts of material. In order to study the robustness of the DDI microarray in determination of IC50 and Kd values, the impact of glycocluster surface density was investigated. The data obtained show that measured IC50 values were influenced by glycocluster surface density: as the density of glycoclusters increases, the measured IC50 values increase too. In contrast, the measured Kd values were not affected by glycocluster surface density, provided that the experimental conditions allow interaction between glycocluster and lectin at single‐molecule level (no surface cluster effect). 相似文献
512.
Novák M Mitchell MJ Jacková I Buzek F Schweigstillová J Erbanová L Prikryl R Fottová D 《Environmental science & technology》2007,41(3):703-709
Sulfate aerosols are harmful as respirable particles. They also play a role as cloud condensation nuclei and have radiative effects on global climate. A combination of delta18O-SO4 data with catchment sulfur mass balances was used to constrain processes affecting S cycling in the atmosphere and spruce forests of the Czech Republic. Extremely high S fluxes via spruce throughfall and runoff were measured at Jezeri (49 and 80 kg S ha(-1) yr(-1), respectively). The second catchment, Na Lizu, was 10 times less polluted. In both catchments, delta18O-SO4 decreased in the following order: open-area precipitation > throughfall > runoff. The delta18O-SO4 values of throughfall exhibited a seasonal pattern at both sites, with maxima in summer and minima in winter. This seasonal pattern paralleled delta18O-H2O values, which were offset by -18 per thousand. Sulfate in throughfall was predominantly formed by heterogeneous (aqueous) oxidation of SO2. Wet-deposited sulfate in an open area did not show systematic delta18O-SO4 trends, suggesting formation by homogeneous (gaseous) oxidation and/or transport from large distances. The percentage of incoming S that is organically cycled in soil was similar under the high and the low pollution. High-temperature 18O-rich sulfate was not detected, which contrasts with North American industrial sites. 相似文献
513.
Callister SJ Wilkins MJ Nicora CD Williams KH Banfield JF VerBerkmoes NC Hettich RL N'Guessan L Mouser PJ Elifantz H Smith RD Lovley DR Lipton MS Long PE 《Environmental science & technology》2010,44(23):8897-8903
Stimulated by an acetate-amendment field experiment conducted in 2007, anaerobic microbial populations in the aquifer at the Rifle Integrated Field Research Challenge site in Colorado reduced mobile U(VI) to insoluble U(IV). During this experiment, planktonic biomass was sampled at various time points to quantitatively evaluate proteomes. In 2008, an acetate-amended field experiment was again conducted in a similar manner to the 2007 experiment. As there was no comprehensive metagenome sequence available for use in proteomics analysis, we systematically evaluated 12 different organism genome sequences to generate sets of aggregate genomes, or "pseudo-metagenomes", for supplying relative quantitative peptide and protein identifications. Proteomics results support previous observations of the dominance of Geobacteraceae during biostimulation using acetate as sole electron donor, and revealed a shift from an early stage of iron reduction to a late stage of iron reduction. Additionally, a shift from iron reduction to sulfate reduction was indicated by changes in the contribution of proteome information contributed by different organism genome sequences within the aggregate set. In addition, the comparison of proteome measurements made between the 2007 field experiment and 2008 field experiment revealed differences in proteome profiles. These differences may be the result of alterations in abundance and population structure within the planktonic biomass samples collected for analysis. 相似文献
514.
Insa Thale Sarah Maskri Lucie Grey Luca Matteo Todesca Prof. Dr. Thomas Budde Dr. Ivan Maisuls Prof. Dr. Cristian A. Strassert Prof. Dr. Oliver Koch Prof. Dr. Albrecht Schwab Prof. Dr. Bernhard Wünsch 《ChemMedChem》2023,18(2):e202200551
The Ca2+ activated K+ channel KCa3.1 is overexpressed in several human tumor cell lines, e. g. clear cell renal carcinoma, prostate cancer, non-small cell lung cancer. Highly aggressive cancer cells use this ion channel for key processes of the metastatic cascade such as migration, extravasation and invasion. Therefore, small molecules, which are able to image this KCa3.1 channel in vitro and in vivo represent valuable diagnostic and prognostic tool compounds. The [18F]fluoroethyltriazolyl substituted senicapoc was used as positron emission tomography (PET) tracer and showed promising properties for imaging of KCa3.1 channels in lung adenocarcinoma cells in mice. The novel senicapoc BODIPY conjugates with two F-atoms ( 9 a ) and with a F-atom and a methoxy moiety ( 9 b ) at the B-atom led to the characteristic punctate staining pattern resulting from labeling of single KCa3.1 channels in A549-3R cells. This punctate pattern was completely removed by preincubation with an excess of senicapoc confirming the high specificity of KCa3.1 labeling. Due to the methoxy moiety at the B-atom and the additional oxyethylene unit in the spacer, 9 b exhibits higher polarity, which improves solubility and handling without reduction of fluorescence quantum yield. Docking studies using a cryo-electron microscopy (EM) structure of the KCa3.1 channel confirmed the interaction of 9 a and 9 b with a binding pocket in the channel pore. 相似文献
515.
Jonas Amft Philipp M. Meissner Anja Steffen-Heins Mario Hasler Heiko Stöckmann Anne Meynier Lucie Birault Joaquín Velasco Ann Vermoesen Ines Perez-Portabella Blanca Prió Tito Porcellana Emanuele Forte Betül Yesiltas Donny Merkx Marie Hennebelle Jianli Wang John van Duynhoven Sonia Losada-Barreiro Carlos Bravo-Diaz Claudio Bernal Helena Abramovič María J. Manzanos Andrea Martínez-Yusta Bárbara Nieva-Echevarría María D. Guillén Sarah Frühwirth Marc Pignitter Rafał Wołosiak Dorota Derewiaka Marlene Costa Fátima Paiva-Martins Charlotte Jacobsen Karin Schwarz 《European Journal of Lipid Science and Technology》2023,125(10):2300067
Accelerated storage tests are frequently used to assess the oxidative stability of foods and related systems due to its reproducibility. Various methods and experimental conditions are used to measure lipid oxidation. Differences between laboratories make it necessary to determine the repeatability and reproducibility of oxidation tests performed under the same conditions. The objective of the present interlaboratory study was to evaluate the outcome of a storage test for two different bulk oils, sunflower oil (SFO) and rapeseed oil (RSO), during a period of 9 weeks at 20°C, 30°C, 40°C, and 60°C. Sixteen laboratories were provided with bottled oils and conducted the storage tests according to a detailed protocol. Lipid oxidation was monitored by the formation of conjugated dienes (CD) and the activation energy (Ea) was determined for comparative purposes and statistically evaluated. An increase in CD formation was observed for both oils when the storage temperature was increased in all laboratories. The Ea,1 ranged from 47.9 to 73.3 kJ mol−1 in RSO and from 27.8 to 62.6 kJ mol−1 in SFO, with average values of 58.2 and 46.8 kJ mol−1, respectively. The reproducibility coefficients were 10.9% and 18.2% for RSO and SFO, respectively. Practical applications: In order to compare results on oxidative stability of foods derived from different studies, the reproducibility of storage tests and methods employed to evaluate the oxidation level should be considered. This study provides fundamental data on the reproducibility of lipid oxidation under accelerated storage conditions and defines important parameters to be considered for the conduction of experiments. 相似文献
516.
David Cluet Blandine Vergier Nicolas-Pierre Levy Lucie Dehau Alexandre Thurman Ikram Amri Martin Spichty 《Chembiochem : a European journal of chemical biology》2022,23(4):e202100640
A genetic assay permits simultaneous quantification of two interacting proteins and their bound fraction at the single-cell level using flow cytometry. Apparent in-cellula affinities of protein-protein interactions can be extracted from the acquired data through a titration-like analysis. The applicability of this approach is demonstrated on a diverse set of interactions with proteins from different families and organisms and with in-vitro dissociation constants ranging from picomolar to micromolar. 相似文献
517.