Chemical Modification of Phage-Displayed Helix-Loop-Helix Peptides to Construct Kinase-Focused Libraries

Conformationally constrained peptides hold promise as molecular tools in chemical biology and as a new modality in drug discovery. The construction and screening of a target-focused library could be a promising approach for the generation of de novo ligands or inhibitors against target proteins. Here, we have prepared a protein kinase-focused library by chemically modifying helix-loop-helix (HLH) peptides displayed on phage and subsequently tethered to adenosine. The library was screened against aurora kinase A (AurA). The selected HLH peptide Bip - 3 retained the α-helical structure and bound to AurA with a K_D value of 13.7 μM. Bip - 3 and the adenosine-tethered peptide Bip - 3 - Adc provided IC₅₀ values of 103 μM and 7.7 μM, respectively, suggesting that Bip - 3 - Adc bivalently inhibited AurA. In addition, the selectivity of Bip - 3 - Adc to several protein kinases was tested, and was highest against AurA. These results demonstrate that chemical modification can enable the construction of a kinase-focused library of phage-displayed HLH peptides.     

A single-solenoid pulsed-magnet system for single-crystal scattering studies

We present a pulsed-magnet system that enables x-ray single-crystal diffraction in addition to powder and spectroscopic studies with the magnetic field applied on or close to the scattering plane. The apparatus consists of a single large-bore solenoid, cooled by liquid nitrogen. A second independent closed-cycle cryostat is used for cooling samples near liquid helium temperatures. Pulsed magnetic fields close to ~30 T with a zero-to-peak-field rise time of ~2.9 ms are generated by discharging a 40 kJ capacitor bank into the magnet coil. The unique characteristic of this instrument is the preservation of maximum scattering angle (~23.6°) on the entrance and exit sides of the magnet bore by virtue of a novel double-funnel insert. This instrument will facilitate x-ray diffraction and spectroscopic studies that are impractical, if not impossible, to perform using split-pair and narrow-opening solenoid magnets. Furthermore, it offers a practical solution for preserving optical access in future higher-field pulsed magnets.     

A Quasi-ARMAX approach to modelling of non-linear systems

This paper proposes a class of quasi-ARMAX models for non-linear systems. Similar to ordinary non-linear ARMAX models, the quasi-ARMAX models are flexible black-box models, but they have various linearity properties similar to those of linear ARMAX models. A modelling scheme is introduced to construct models consisting of two parts: a macro-part and a kernel-part. By using Taylor expansion and other mathematical transformation techniques, it is first constructed as a class of quasi-ARMAX interfaces (macro-parts) that have various linearity properties but contain some complicated coefficients. MIMO neurofuzzy models (kernel-parts) are then introduced to represent the complicated coefficients. It is shown that the proposed quasi-ARMAX models have both good approximation ability and some easy-to-use properties. The proposed models have been successfully applied to prediction, fault detection and adaptive control of non-linear systems.     

Immobilization of alkaline phosphatase on magnetic particles by site-specific and covalent cross-linking catalyzed by microbial transglutaminase

Bacterial alkaline phosphatase (BAP) was site-specifically and covalently immobilized on magnetic particles (MPs) using the enzymatic reaction of microbial transglutaminase (MTG). Immobilization efficiency was affected by the chemical surface treatment of MPs and immobilized BAP exhibited more than 90% of the initial activity after 10 rounds of recycling.     

Distribution, characteristics, and worldwide inventory of dioxins in kaolin ball clays

Distribution, characteristics, and global inventory of dioxins (polychlorinated dibenzo-p-dioxins [PCDDs] and dibenzofurans [PCDFs] and dioxin like polychlorinated biphenyls) in kaolin clays collected from 10 countries were investigated. Dioxins were found in all kaolin clay samples analyzed, at total concentrations ranging from 1.2 pg/g (Brazil) to 520,000 pg/g (USA). Dioxin concentrations in kaolin clays from a few countries (e.g., Brazil and UK) were lower than those reported for background soils in Japan. Dioxin profiles in kaolin clays were characterized by the domination of the congener octachlorodibenzo-p-dioxin (OCDD), and the concentrations of other congeners decreased in the order of reduction in the levels of chlorination. Furthermore, specific distribution of congeners, with predominant proportions of 1,4,6,9-substituted PCDDs within each homologue group, was found in most clay samples. The ratios of concentrations of PCDD to PCDF and 1,2,3,7,8,9-HxCDD to 1,2,3,6,7,8-HxCDD indicated differences in the profiles found for anthropogenic sources (including pentachlorophenol) and kaolin clays. Concentrations of PCDD/Fs in kaolin clays, except for American ball clays, did not exceed the environmental criteria set by the Law Concerning Special Measures against Dioxins in Japan. Based on the average concentrations measured in our study, inventories of PCDD/Fs from the production/usage of ball clays on a global scale were estimated to be 650 kg/yr; the corresponding value on a TEQ basis is 2400 g-TEQ/yr. More than 480 kg of OCDD is estimated to be released annually from the production of kaolin clays worldwide, suggesting that kaolin clays can be a major contributor for additional source of dioxins, especially OCDD, in the environment.     

Simultaneous determination of five antioxidants in food by HPLC with fluorescence detection

An HPLC method with fluorescence detection was developed for the determination of propyl gallate, nordihydroguaiaretic acid, butylated hydroxyanisole (2- and 3-tert-butyl-4-hydroxyanisole), tert-butylhydroquinone and octyl gallate in edible oils and foods. The antioxidants in edible oil were isolated directly with acetonitrile saturated with n-hexane. The antioxidants in food were extracted with ethyl acetate and the extract was concentrated under vacuum. They were isolated from the residue with acetonitrile saturated with n-hexane. The acetonitrile layer was centrifuged at 5,000 rpm for 10 min. The HPLC separation was performed on a Symmetry C18 column (3.5 microns, 4.6 mm i.d. x 150 mm) using a mixture of 5% acetic acid-acetonitrile-methanol (4:3:3, v/v/v) as the mobile phase and monitored by using a fluorescence detector with time programming. Sample peaks were identified by comparison of the fluorescence spectra with those of antioxidant standards. Average recoveries of fortified antioxidants at 100 micrograms/g were 72.1-99.6%. Coefficients of variation were 0.7-7.2%.     

Liquid‐phase sintering of highly Na+ ion conducting Na3Zr2Si2PO12 ceramics using Na3BO3 additive

Na₃Zr₂Si₂PO₁₂ (NASICON) is a promising material as a solid electrolyte for all‐solid‐state sodium batteries. Nevertheless, one challenge for the application of NASICON in batteries is their high sintering temperature above 1200°C, which can lead to volatilization of light elements and undesirable side reactions with electrode materials at such high temperatures. In this study, liquid‐phase sintering of NASICON with a Na₃BO₃ (NBO) additive was performed for the first time to lower the NASICON sintering temperature. A dense NASICON‐based ceramic was successfully obtained by sintering at 900°C with 4.8 wt% NBO. This liquid‐phase sintered NASICON ceramic exhibited high total conductivity of ~1 × 10^?3 S cm^?1 at room temperature and low conduction activation energy of 28 kJ mol^?1. Since the room‐temperature conductivity is identical to that of conventional high‐temperature‐sintered NASICON, NBO was demonstrated as a good liquid‐phase sintering additive for NASICON solid electrolyte. In the NASICON with 4.8 wt% NBO ceramic, most of the NASICON grains directly bonded with each other and some submicron sodium borates segregated in particulate form without full penetration to NASICON grain boundaries. This characteristic composite microstructure contributed to the high conductivity of the liquid‐phase sintered NASICON.     

Criteria for versatile GaN MOVPE tool:high growth rate GaN by atmospheric pressure growth

Growth rate has a direct impact on the productivity of nitride LED production.Atmospheric pressure growth of GaN with a growth rate as high as 10μm/h and also Al_0.1Ga_0.9N growth of 1μm/h by using 4 inch by 11 production scale MOVPE are described.XRD of（002） and（102） direction was 200 arcsec and 250 arcsec, respectively.Impact of the growth rate on productivity is discussed.     

Oxygen release behavior of metastable tetragonal t′meta-(Ce0.5Zr0.5)2 phases prepared by reduction and successive oxidation of t′ phase

Tetragonal CaF₂-related-type t′-/Ce_0.5Zr_0.5)O₂ phase was reduced at 773 K ≤ T_red. ≤ 1073 K to prepare precursors with various oxygen compositions: Ce₂Zr₂O_712d /0.111 < δ < 0.379). Metastable tetragonal t^′_meta-(Ce_0.5Zr_0.5)O₂ phases were prepared by oxidizing in O₂ at 873 K the precursors, and subjected to evolved oxygen gas analysis by heating the samples at a constant rate. When the precursor was prepared at T_red: ? 773 K; i.e. δ ? 0:379; the oxygen release behavior of the tetragonal phase agreed approximately with that of the t^′. For δ < 0.29, distinct features of the t^′_meta-(Ce_0.5Zr_0.5)O₂ appeared in the XRD results and Raman spectra. The temperature exhibiting the maximum release rate of oxygen from the t^′_meta became lower with decreasing the d value. It could be concluded that the thermodynamic behavior of the t^′_meta is related closely to the precursor composition and becomes more unstable with decrease in the δ value. The t^′ and t^′_meta phases with disordered arrangement of Ce and Zr ions may belong to the same space group; nevertheless, difference in the random arrays of the Ce and Zr ions was suggested on the basis of the present experimental results.     

Synthesis of charge transporting block copolymers containing 2,7-dimethoxycarbazole units for light emitting device

The block copolymers consisting of 2,7-dimethoxycarbazole- and oxadiazole-containing segments as hole and electron transporting units, respectively, were synthesized by NMRP manner. OLED devices were fabricated using block copolymer, random copolymer, and polymer blend for matrix of the emitting layer with Ir(ppy)₃ as a phosphorescent dopant in order to investigate morphological effect on the performance. From the finding that the block copolymer system overwhelmed the others in EQE, we assumed that a morphology with dimethoxycarbazole units assembled to the surface of PEDOT:PSS played a considerable role for effective recombination of charges as well as sufficient charge injection into the emitting layer.