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排序方式: 共有145条查询结果,搜索用时 15 毫秒
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Jonker N Kool J Krabbe JG Retra K Lingeman H Irth H 《Journal of chromatography. A》2008,1205(1-2):71-77
A novel methodology is shown enabling the screening of mixtures of compounds for their affinity to a receptor protein. The system presented, dynamic protein-affinity chromatography solid-phase extraction (DPAC-SPE), overcomes the limitations of the existing methods by performing an incubation of the His-tagged protein with a mixture of possible ligands, which are still in their native conditions. This is followed by a fully automated affinity trapping step, coupled on-line to an LC-MS system in order to detect and identify the bound ligands. The system has been optimized using a commercially available on-line SPE system, using the estrogen receptor alpha (ERalpha) as model protein. A representative range of ligands with sub-nanomolar to millimolar affinities has been identified successfully from a mixture. The weakest binder that can be identified is norethindrone (approximately K(d)=0.1-1mM). The same setup also provides the possibilities to measure EC50 curves of both weak and strong binders. 相似文献
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We report synthetically accessible receptors with protonated amines attached to a conformationally constrained backbone including amide units, and demonstrate that these receptors have high affinities (log K > 5) for phosphate anions in aqueous media at pH 7 in the presence of high concentrations of competitive chloride anions (ca. 100-fold excess). 相似文献
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High-performance liquid chromatography-mass spectrometry-based acetylcholinesterase assay for the screening of inhibitors in natural extracts 总被引:1,自引:0,他引:1
de Jong CF Derks RJ Bruyneel B Niessen W Irth H 《Journal of chromatography. A》2006,1112(1-2):303-310
The present paper describes a High-performance liquid chromatography-mass spectrometry (LC-MS) methodology for the screening of acetylcholinesterase (AChE) inhibitors in natural extracts. AChE activity of sample components is monitored by a post-column biochemical assay that is based on the separate, sequential mixing of AChE and acetylcholine, respectively, with the HPLC eluate. AChE inhibitors are detected by measuring a decrease of product formation using electrospray MS. Ammonium bicarbonate was used as buffer in order to achieve optimum compatibility between biochemical assay and MS detection conditions. The assay is robust and stable for over 13 h and compares favourably with other AChE assays in terms of stability and sensitivity. IC(50) values of 9-aminoacridine, galanthamine, gallamine, (-)-huperzine A and thioflavin T were determined to be 0.12, 0.38, 6.4, 0.46 and 3.2 microM, respectively. The assay was used to effectively identify an AChE inhibitor present in a crude extract of Narcissus c.v. "Bridal Crown". 相似文献
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CW Yeh WT Chen RS Liu SF Hu HS Sheu JM Chen HT Hintzen 《Journal of the American Chemical Society》2012,134(34):14108-14117
The orange-red emitting phosphors based on M(2)Si(5)N(8):Eu (M = Sr, Ba) are widely utilized in white light-emitting diodes (WLEDs) because of their improvement of the color rendering index (CRI), which is brilliant for warm white light emission. Nitride-based phosphors are adopted in high-performance applications because of their excellent thermal and chemical stabilities. A series of nitridosilicate phosphor compounds, M(2-x)Si(5)N(8):Eu(x) (M = Sr, Ba), were prepared by solid-state reaction. The thermal degradation in air was only observed in Sr(2-x)Si(5)N(8):Eu(x) with x = 0.10, but it did not appear in Sr(2-x)Si(5)N(8):Eu(x) with x = 0.02 and Ba analogue with x = 0.10. This is an unprecedented investigation to study this phenomenon in the stable nitrides. The crystal structural variation upon heating treatment of these compounds was carried out using the in situ XRD measurements. The valence of Eu ions in these compounds was determined by electron spectroscopy for chemical analysis (ESCA) and X-ray absorption near-edge structure (XANES) spectroscopy. The morphology of these materials was examined by transmission electron microscopy (TEM). Combining all results, it is concluded that the origin of the thermal degradation in Sr(2-x)Si(5)N(8):Eu(x) with x = 0.10 is due to the formation of an amorphous layer on the surface of the nitride phosphor grain during oxidative heating treatment, which results in the oxidation of Eu ions from divalent to trivalent. This study provides a new perspective for the impact of the degradation problem as a consequence of heating processes in luminescent materials. 相似文献
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K Bhaskaran-Nair J Brabec E Aprà HJ van Dam J Pittner K Kowalski 《The Journal of chemical physics》2012,137(9):094112
In this paper we discuss the performance of the non-iterative state-specific multireference coupled cluster (SS-MRCC) methods accounting for the effect of triply excited cluster amplitudes. The corrections to the Brillouin-Wigner and Mukherjee's MRCC models based on the manifold of singly and doubly excited cluster amplitudes (BW-MRCCSD and Mk-MRCCSD, respectively) are tested and compared with exact full configuration interaction results for small systems (H(2)O, N(2), and Be(3)). For the larger systems (naphthyne isomers) the BW-MRCC and Mk-MRCC methods with iterative singles, doubles, and non-iterative triples (BW-MRCCSD(T) and Mk-MRCCSD(T)) are compared against the results obtained with single reference coupled cluster methods. We also report on the parallel performance of the non-iterative implementations based on the use of processor groups. 相似文献
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Axisymmetric deformations of annular membranes subjected to normal surface loads and radial edge loads or displacements are considered within the Föppl nonlinear membrane theory. When the inner edger=a is free of radial traction, the solution of the annular membrane problem is shown to reduce to the solution for the circular membrane (a=0). For nonvanishing traction atr=a, the problem is reduced to a circular pseudo-membrane problem. For both cases, existence and uniqueness of tensile solutions of the annular membrane problem are proved, including a rigorous derivation of a stress concentration factor originally found by Schwerin by formal methods. 相似文献