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Johan F. A. Pijnenborg Eline A. Visser Dr. Marek Noga Emiel Rossing Raisa Veizaj Prof. Dirk J. Lefeber Dr. Christian Büll Dr. Thomas J. Boltje 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(12):4022-4027
Fucosylation of glycans impacts a myriad of physiological and pathological processes. Inhibition of fucose expression emerges as a potential therapeutic avenue for example in cancer, inflammation, and infection. In this study, we found that protected 2-fluorofucose 1-phosphate efficiently inhibits cellular fucosylation with a four to seven times higher potency than known inhibitor 2FF, independently of the anomeric stereochemistry. Nucleotide sugar analysis revealed that both the α- and β-GDP-2FF anomers are formed inside the cell. In conclusion, we developed A2FF1P and B2FF1P as potent new tools for studying the role of fucosylation in health and disease and they are potential therapeutic candidates. 相似文献
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Platinum‐Promoted Ga/Al2O3 as Highly Active,Selective, and Stable Catalyst for the Dehydrogenation of Propane
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Jesper J. H. B. Sattler Dr. Ines D. Gonzalez‐Jimenez Dr. Lin Luo Brien A. Stears Dr. Andrzej Malek Dr. David G. Barton Dr. Beata A. Kilos Dr. Mark P. Kaminsky Tiny W. G. M. Verhoeven Eline J. Koers Prof. Dr. Marc Baldus Prof. Dr. Bert M. Weckhuysen 《Angewandte Chemie (International ed. in English)》2014,53(35):9251-9256
A novel catalyst material for the selective dehydrogenation of propane is presented. The catalyst consists of 1000 ppm Pt, 3 wt % Ga, and 0.25 wt % K supported on alumina. We observed a synergy between Ga and Pt, resulting in a highly active and stable catalyst. Additionally, we propose a bifunctional active phase, in which coordinately unsaturated Ga3+ species are the active species and where Pt functions as a promoter. 相似文献
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Sebastian Schlund Eline M. Basílio Janke Klaus Weisz Bernd Engels 《Journal of computational chemistry》2010,31(4):665-670
This study investigates how the various components (method, basis set, and treatment of solvent effects) of a theoretical approach influence the relative energies between keto and enol forms of acetylacetone, which is an important model system to study the solvent effects on chemical equilibria from experiment and theory. The computations show that the most popular density functional theory (DFT) approaches, such as B3LYP overestimate the stability of the enol form with respect to the keto form by ~10 kJ mol?1, whereas the very promising SCS‐MP2 approach is underestimating it. MP2 calculations indicate that in particular the basis set size is crucial. The Dunning Huzinaga double ζ basis (D95z(d,p)) used in previous studies overestimates the stability of the keto form considerably as does the popular split‐valence plus polarization (SVP) basis. Bulk properties of the solvent included by continuum approaches strongly stabilize the keto form, but they are not sufficient to reproduce the reversal in stabilities measured by low‐temperature nuclear magnetic resonance experiments in freonic solvents. Enthalpic and entropic effects further stabilize the keto form, however, the reversal is only obtained if also molecular effects are taken into account. Such molecular effects seem to influence only the energy difference between the keto and the enol forms. Trends arising due to variation in the dielectric constant of the solvent result from bulk properties of the solvent, i.e., are already nicely described by continuum approaches. As such this study delivers a deep insight into the abilities of various approaches to describe solvent effects on chemical equilibria. © 2009 Wiley Periodicals, Inc. J Comput Chem, 2010 相似文献
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In this paper, the point-distance-2-regular hexagons are characterized as the only hexagons for which the intersection sets have size one and containing on ovoidal subspace all the points of which are 3-regular. We also give a characterization of the finite split Cayley hexagon of even order. 相似文献
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Berry DJ Ma Y Ballinger JR Tavaré R Koers A Sunassee K Zhou T Nawaz S Mullen GE Hider RC Blower PJ 《Chemical communications (Cambridge, England)》2011,47(25):7068-7070
A new tripodal tris(hydroxypyridinone) bifunctional chelator for gallium allows easy production of (68)Ga-labelled proteins rapidly under mild conditions in high yields at exceptionally high specific activity and low concentration. 相似文献
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Rationally Designed Semisynthetic Natural Product Analogues for Stabilization of 14‐3‐3 Protein–Protein Interactions
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Sebastian A. Andrei Pim de Vink Eline Sijbesma Ling Han Prof. Luc Brunsveld Prof. Nobuo Kato Prof. Christian Ottmann Dr. Yusuke Higuchi 《Angewandte Chemie (International ed. in English)》2018,57(41):13470-13474
The natural product family of fusicoccanes are stabilizers of 14‐3‐3 mediated protein–protein interactions (PPIs), some of which possess antitumor activity. In this study, the first use of molecular dynamics (MD) to rationally design PPI stabilizers with increased potency is presented. Synthesis of a focused library, with subsequent characterization by fluorescence polarization, mutational studies, and X‐ray crystallography confirmed the power of the MD‐based design approach, revealing the potential for an additional hydrogen bond with the 14‐3‐3 protein to lead to significantly increased potency. Additionally, these compounds exert their action in a cellular environment with increased potency. The newly found polar interaction could provide an anchoring point for new small‐molecule PPI stabilizers. These results facilitate the development of fusicoccanes towards drugs or tool compounds, as well as allowing the study of the fundamental principles behind PPI stabilization. 相似文献
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Planar electrochromatography is performed by applying an electric field across a thin layer chromatography (TLC) plate. In addition to electroosmotic flow in the axial direction, there is also flow to the surface of the TLC layer, and this can substantially degrade the quality of separation. This effect is offset by Joule heating which causes evaporation of liquid from the layer surface, and which under some conditions causes degradation of separation quality by excessive drying of the layer. It is shown that pH, buffer concentration, and applied voltage control the balance between liquid being driven to the surface and liquid evaporating from the surface due to Joule heating. Conditions are discussed which result in good separation quality, or in separations degraded by either excessive wetting or drying of the layer. The above separations were performed at constant voltage. A chromatogram is presented that shows that a good separation is also obtained at constant power, i.e. under conditions where there is a constant amount of Joule heating. 相似文献
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