Probing the Conformation States of Neurotensin Receptor 1 Variants by NMR Site-Directed Methyl Labeling

G protein-coupled receptors (GPCRs) are key players in mediating signal transduction across the cell membrane. However, due to their intrinsic instability, many GPCRs are not suitable for structural investigations. Various approaches have been developed in recent years to remedy this situation, ranging from the use of more native membrane mimetics to protein-stabilization methods. The latter approach typically results in GPCRs that contain various numbers of mutations. However, probing the functionality of such variants by in vitro and in vivo assays is often time consuming. In addition, to validate the suitability of such GPCRs for structural investigations, an assessment of their conformation state is required. NMR spectroscopy has been proven to be suitable to probe the conformation state of GPCRs in solution. Here, by using chemical labeling with an isotope-labeled methyl probe, we show that the activity and the conformation state of stabilized neurotensin receptor 1 variants obtained from directed evolution can be efficiently assayed in 2D NMR experiments. This strategy enables the quantification of the active and inactive conformation states and the derivation of an estimation of the basal as well as agonist-induced activity of the receptor. Furthermore, this assay can be used as a readout when re-introducing agonist-dependent signaling into a highly stabilized, and thus rigidified, receptor by mutagenesis. This approach will be useful in cases where low production yields do not permit the addition of labeled compounds to the growth medium and where 1D NMR spectra of selectively ¹⁹F-labeled receptors are not sufficient to resolve signal overlap for a more detailed analysis.     

Processing of High-Density Submicrometer Al2O3 for New Applications

Sintered corundum components with submicrometer grain sizes exhibit properties which enable numerous new applications. Wet powder processing is developed to associate minimum grain sizes at highest densities with the lowest population of macrodefects. A closest ratio of powder particle size and sintered grain size is important for obtaining most fine-grained microstructures. This target was approached best by using powders with particle sizes in the range of 100–200 nm rather than with smaller nanoparticles.     

High Throughput Screening of Low Temperature SCR and SCD De-NOx Catalysts in Scanning Mass Spectrometer

High-throughput synthesis and screening methods have been developed for the discovery of highly active lead compounds for the selective catalytic reduction as well as direct decomposition of NO in the temperature range 200–300 °C. The discovery libraries for primary screening consisted of 16 × 16 catalyst arrays on 4in. square quartz wafers. Catalysts were prepared by robotic liquid dispensing techniques and screened for catalytic activity in Symyx' scanning mass spectrometer. The scanning mass spectrometer is a fast serial screening tool that uses flat wafer catalyst surfaces, local laser heating, a scanning/sniffing nozzle and a quadrupolar mass spectrometer to compare relative catalytic activities. The feed consisted of NO/NH₃ mixtures with optional O₂ cofeed and Kr as the internal standard in Ar carrier gas. QMS detection allowed for tracking of H₂O, N₂, NO, O₂, N₂O and Kr. Screening protocols for catalytic materials encompassed metal precursors and carriers for supported vanadia systems, extensive doping of V₂O₅/TiO₂, and broad screening of mixed redox metal oxides and supported base and noble metal systems. More than 500 samples could be screened in a single day. Active hits (high NO consumption accompanied by corresponding N₂ production) identified in discovery libraries were re-synthesized as focus libraries for lead confirmation and further optimization. These libraries used shallower compositional gradients, for example 56 points (compositions) per ternary, with four 56-point ternaries per 4in. wafer. Broad screening ternaries were generally 8 or 15 points. The focus libraries more clearly reveal the trends and provide guidelines for secondary screening and scale-up. High conversions were achieved in scanning mass spectrometer so the scalability risk is small for the short contact time reactions.     

Syntheses of TiO2 photocatalysts by the molten salts method: Application to the photocatalytic degradation of Prosulfuron

Titania photocatalysts were synthesised by the molten salts method by reaction of a titanium precursor with three different alkali metal nitrates (LiNO₃, NaNO₃, KNO₃). The titania powders obtained have been characterised using TEM, XRD, BET and UV-Vis absorption spectroscopy. Their photoactivities were evaluated by degrading a commercial sulfonylurea herbicide, Prosulfuron^®. It has been found that the rate constants increased in the following order: Li2 prepared in KNO₃, with a rate constant 1.4 times smaller than that of P25. The effect of calcination was also studied, especially for the sample prepared in NaNO₃ (TiO₂[Na]). An improvement in photocatalytic activity was observed when TiO₂[Na] was calcined in the region of 700–800 °C. Even though the photocatalytic activities obtained did not exceed or even equal to that of Degussa P25, nevertheless, this study constitutes the first attempt to synthesise titania photocatalysts by the molten salts method.     

阳极氧化铝的表面参数对硅酮结构的装锒密封胶长期黏结性的影响(连载一)

硅酮密封胶对阳极氧化铝的黏结质量千差万别.影响黏结性的关键因素是铝材表面的封孔程度、氧化层的着色情况、清洁剂的特性以及基材表面清洁与打胶之间允许的时间间隔.由于清洁剂将有机污染物从阳极氧化铝表面去除的效果不同,所以此效果并不和黏结质量有必然联系.据猜测,吸附在阳极氧化铝表面的清洁溶剂会改善基材表面从而提高硅酮胶的黏结性,但这种改善效果会随着清洁溶剂随时间的的挥发而降低.对于给定的溶剂,最佳的黏结效果取决于材料表面的封孔程度.依照ISO 2143酸刻蚀方法测量材料表面的封孔程度,可以预测未着色的阳极氧化铝基材的黏结性.对于着色的阳极氧化铝表面,依照ISO 2931的测试标准,用电相位漂移方法可以用来预测黏结质量.一种控制阳极氧化铝表面的方法被提了出来,此方法是测量不同频率下基材的电阻抗并将它成功地和硅酮密封胶与该材料表面的长期黏接性联系起来.     

Influence of compaction on the interfacial transition zone and the permeability of concrete

The interfacial transition zone (ITZ) is regarded as a key feature for the transport properties and the durability of concrete. In this study one self-compacting concrete (SCC) mixture and two conventionally vibrated concrete (CVC) mixtures are studied in order to determine the influence of compaction on the porosity of the ITZ. Additionally oxygen permeability and water conductivity were measured in vertical and horizontal direction. The quantitative analysis of images made with an optical microscope and an environmental scanning electron microscope shows a significantly increased porosity and width of the ITZ in CVC compared to SCC. At the same time oxygen permeability and water conductivity of CVC are increased in comparison to SCC. Moreover, considerable differences in the porosity of the lower, lateral and upper ITZ are observed in both types of concrete. The anisotropic distribution of pores in the ITZ does not necessarily cause anisotropy in oxygen permeability and water conductivity though.     

GestIC~ Overkey~(3D)——Windows~ 8环境下的自由空间键盘控制

正早在20世纪90年代,触摸板就已作为笔记本电脑的用户接口出现了。今天,触摸板已大规模替代轨迹球和操控手柄。触摸技术已经升级到了电容式触摸传感,并且其功能已囊括多点触摸。尽管在过去的20年里触摸板技术有了长足的发展,但由于安装条件有限,并且触摸板需要大约5 mm~7 mm的厚度,这些仍然限制     

Trends beim Einsatz von Realzeitrechnern für Forschung und Entwicklung in der Technischen Chemie

Trends in the use of real-time computers for research and development in industrial chemistry. Computers are integral parts of the complex equipment of chemical production plants. They are tools for computer aided process control. In production plants as well as in research and development laboratories, dedicated computer systems are used more and more. E. g., nearly all measuring devices will be controlled by their own microprocessors in the near future. In chemical engineering, however, the most significant developments are taking place in the software domain. The main trend in applications-software developments is the enhanced importance of the support of the plant operators by means of improved user interfaces. Within the research and development field, the software must be more flexibly adaptable to changes in the process equipment and due to changing control algorithms than in production plants. Moreover, efforts are being made to improve control by exploiting as much as possible a priori knowledge on the system in question. A current development in this direction, which will become stronger with time, is known under the heading ?expert systems”?, in which heuristic know-how of operators is made available and usable in process computers to improve control.     

Jet bundle formulation of infinite-dimensional port-Hamiltonian systems using differential operators

We consider infinite-dimensional port-Hamiltonian systems described on jet bundles. Based on a power balance relation we introduce the port-Hamiltonian system representation using differential operators regarding the structural mapping, the dissipation mapping and the input mapping. In contrast to the well-known representation on the basis of the underlying Stokes–Dirac structure our approach is not necessarily based on using energy-variables which leads to a different port-Hamiltonian representation of the analyzed partial differential equations. The presented constructions will be specialized to mechanical systems to which class also the presented examples belong.