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71.
Dr. Hui Qiu Richard Caldwell Dr. Lesley Liu-Bujalski Dr. Andreas Goutopoulos Reinaldo Jones Justin Potnick Dr. Brian Sherer Dr. Andrew Bender Dr. Roland Grenningloh Dr. Daigen Xu Dr. Anna Gardberg Dr. Igor Mochalkin Dr. Theresa Johnson Dr. Ariele Viacava Follis Jared Head Dr. Federica Morandi 《ChemMedChem》2019,14(2):217-223
Bruton's tyrosine kinase (Btk) is an attractive target for the treatment of a wide array of B-cell malignancies and autoimmune diseases. Small-molecule covalent irreversible Btk inhibitors targeting Cys481 have been developed for the treatment of such diseases. In clinical trials, probe molecules are required in occupancy studies to measure the level of engagement of the protein by these covalent irreversible inhibitors. The result of this pharmacodynamic (PD) activity provides guidance for appropriate dosage selection to optimize inhibition of the drug target and correlation of target inhibition with disease treatment efficacy. This information is crucial for successful evaluation of drug candidates in clinical trials. Based on the pyridine carboxamide scaffold of a novel solvent-accessible pocket (SAP) series of covalent irreversible Btk inhibitors, we successfully developed a potent and selective affinity-based biotinylated probe 12 (2-[(4-{4-[5-(1-{5-[(3aS,4S,6aR)-2-oxo-hexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanamido}-3,6,9,12-tetraoxapentadecan-15-amido)pentanoyl]piperazine-1-carbonyl}phenyl)amino]-6-[1-(prop-2-enoyl)piperidin-4-yl]pyridine-3-carboxamide). Compound 12 has been used in Btk occupancy assays for preclinical studies to determine the therapeutic efficacy of Btk inhibition in two mouse lupus models driven by TLR7 activation and type I interferon. 相似文献
72.
73.
David J. Lawrence Brianna L. Smith Cameron D. Collard Keyton A. Elliott Kyle L. Fakhoury Jeffery D. Mangold Anna N. Soyka 《International Journal of Hydrogen Energy》2021,46(2):1642-1655
Monolithically-integrated tandem photoanodes were fabricated on substrates consisting of epitaxial n-GaAs1-xPx (x ? 0.32) grown on n+-GaAs wafers. A p+-n junction photovoltaic (PV) cell was first formed by zinc diffusion into the n-GaAs0.68P0.32 from a deposited ZnO coating. After diffusion the ZnO serves as a transparent electrical contact to the resulting p+-GaAs0.68P0.32 surface layer. Transparent, conducting SnO2:F provides chemical and mechanical protection for the ZnO and the underlying PV cell, and it electrically connects this cell to a top BiVO4 photocatalyst layer. In some photoanodes, a WO3 thin film was interposed between the SnO2:F and BiVO4. All oxide coatings were produced by ultrasonic spray pyrolysis except WO3, which was spin coated. Unassisted (unbiased) solar water splitting was achieved, with a solar-to-hydrogen efficiency approaching 2%, without addition of any co-catalyst to the BiVO4 surface. This work can provide insights to other researchers regarding scalable, low cost approaches for the planar monolithic integration of oxide photoanode materials with PV cells to create new tandem devices. 相似文献
74.
Kinetic,thermodynamic parameters and in vitro digestion of tannase from Aspergillus tamarii URM 7115
Amanda Reges de Sena Tonny Cley Campos Leite Talita Camila Evaristo da Silva Nascimento Anna Carolina da Silva Catiane S. Souza Antônio Fernando de Mello Vaz 《Chemical Engineering Communications》2018,205(10):1415-1431
Tannase is an enzyme used in various industries and produced by a large number of microorganisms. The aim of this study was to evaluate tannase production to determine the biochemical, kinetic, and thermodynamic properties and to simulate tannase in vitro digestion. The tannase-producing fungal strain was isolated from “jamun” leaves and identified as Aspergillus tamarii. Temperature at 26°C for 67?h was the best combination for maximum tannase activity (6.35-fold; initial activity in Plackett–Burman design—15.53?U/mL and average final activity in Doehlert design—98.68?U/mL). The crude extract of tannase was optimally active at 40°C, pH 5.5 and 6.5. Moreover, tannase was stimulated by Na+, Ca2+, Mg2+, and Mn2+. The half-life at 40°C lasted 247.55?min. The free energy of Gibbs, enthalpy, and entropy, at 40°C, was 81.47, 16.85, and ?0.21?kJ/mol?·?K, respectively. After total digestion, 123.95% of the original activity was retained. Results suggested that tannase from A. tamarii URM 7115 is an enzyme of interest for industrial applications, such as gallic acid production, additive for feed industry, and for beverage manufacturing, due to its catalytic and thermodynamic properties. 相似文献
75.
76.
Meza-Espinoza Libier de los Ángeles Vivar-Vera María de Lourdes García-Magaña María Sáyago-Ayerdi Sonia G. Chacón-López Alejandra Becerrea-Verdín Eduardo M. Montalvo-González Efigenia 《Food science and biotechnology》2018,27(2):509-517
Food Science and Biotechnology - The enzymatic activity and partial characterization of proteases from Bromelia karatas fruits were evaluated and compared with Bromelia pinguin proteases. The... 相似文献
77.
Real-time multimedia applications have to use forward error correction (FEC) anderror concealment techniques to cope with
losses in today’s best-effort Internet. The efficiency of these solutions is known however to depend on the correlation between
losses in the media stream. In this paper we investigate how the packet size distribution affects the packet loss process,
that is, the distribution of the number of lost packets in a block, the related FEC performance and the average loss run length.
We present mathematical models for the loss process of the MMPP+M/D/1/K and the MMPP+M/M/1/K queues; we validate the models
via simulations, and compare the results to simulation results with an MPEG-4 coded video trace. We conclude that the deterministic
packet size distribution (PSD) not only results in lower stationary loss probability than the exponential one, but also gives
a less correlated loss process, both at a particular average link load and at a particular stationary loss probability as
seen by the media stream.Our results show that for applications that can only measure the packet loss probability, the effects
of the PSD on FEC performance are higher in access networks, where a single multimedia stream might affect the multiplexing
behavior. Our results show that the effects of the PSD on FEC performance are higher in access networks, where a single multimedia
stream might affect the multiplexing behavior and thus can improve the queuing performance by decreasing the variance of its
PSD. 相似文献
78.
Kruk Menno R.; Halász József; Meelis Wout; Haller József 《Canadian Metallurgical Quarterly》2004,118(5):1062
Aggressive behavior induces an adrenocortical stress response, and sudden stressors often precipitate violent behavior. Experiments in rats revealed a fast, mutual, positive feedback between the adrenocortical stress response and a brain mechanism controlling aggression. Stimulation of the aggressive area in the hypothalamus rapidly activated the adrenocortical response, even in the absence of an opponent and fighting. Hypothalamic aggression, in turn, was rapidly facilitated by a corticosterone injection in rats in which the natural adrenocortical stress response was prevented by adrenalectomy. The rapidity of both effects points to a fast, mutual, positive feedback of the controlling mechanisms within the time frame of a single conflict. Such a mutual facilitation may contribute to the precipitation and escalation of violent behavior under stressful conditions. (PsycINFO Database Record (c) 2010 APA, all rights reserved) 相似文献
79.
Eduardo Freire Teodiano Bastos-Filho Mário Sarcinelli-Filho Ricardo Carelli 《IEEE transactions on systems, man, and cybernetics. Part B, Cybernetics》2004,34(1):419-429
This paper proposes an alternative approach to address the problem of coordinating behaviors in mobile robot navigation: fusion of control signals. Such approach is based on a set of two decentralized information filters, which accomplish the data fusion involved. Besides these two fusion engines, control architectures designed according to this approach also embed a set of different controllers that generate reference signals for the robot linear and angular speeds. Such signals are delivered to the two decentralized information filters, which estimate suitable overall reference signals for the robot linear and angular speeds, respectively. Thus, the background for designing such control architectures is provided by the nonlinear systems theory, which makes this approach different from any other yet proposed. This background also allows checking control architectures designed according to the proposed approach for stability. Such analysis is carried out in the paper, and shows that the robot always reaches its final destination, in spite of either obstacles along its path or the environment layout. As an example, a control architecture is designed to guide a mobile robot in an experiment, whose results allows checking the good performance of the control architecture and validating the design approach proposed as well. 相似文献
80.
A comprehensive study of hazelnut oil composition with comparisons to other vegetable oils,particularly olive oil. 总被引:4,自引:0,他引:4
Benitez-Sánchez Pedro Luis León-Camacho Manuel Aparicio Ramón 《European Food Research and Technology》2003,218(1):13-19
Crude and refined hazelnut oils from different countries were characterised by major and minor compounds. Fatty acids, triacylglycerides, waxes, sterols, methyl-sterols, terpenic and aliphatic alcohols, tocopherols, tocotrienols and hydrocarbons were identified and quantified by gas chromatography and high-performance liquid chromatography. The levels of these chemical compounds in hazelnut oils together with the equivalent carbon numbers and triacylglyceride carbon numbers, were compared with the results of analyses of samples of other vegetable oils. The statistical procedure of cluster analysis was used to characterise hazelnut oils versus other edible oils. 相似文献