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21.
We describe here an extensive structure-bioluminescence relationship study of a chemical library of analogues of coelenterazine, using nanoKAZ/NanoLuc, a mutated luciferase originated from the catalytic subunit of the deep-sea shrimp Oplophorus gracilirostris. Out of the 135 O-acetylated precursors that were prepared by using our recently reported synthesis and following their hydrolysis to give solutions of the corresponding luciferins, notable bioluminescence improvements were achieved in comparison with furimazine, which is currently amongst the best substrates of nanoKAZ/NanoLuc. For instance, the rather more lipophilic analogue 8-(2,3-difluorobenzyl)-2-((5-methylfuran-2-yl)methyl)-6-phenylimidazo[1,2-a]pyrazin-3(7H)-one provided a 1.5-fold improvement of the total light output over a 2 h period, a close to threefold increase of the initial signal intensity and a signal-to-background ratio five times greater than furimazine. The kinetic parameters for the enzymatic reaction were obtained for a selection of luciferin analogues and provided unexpected insights into the luciferase activity. Most prominently, along with a general substrate-dependent and irreversible inactivation of this enzyme, in the case of the optimized luciferin mentioned above, the consumption of 2664 molecules was found to be required for the detection of a single Relative Light Unit (RLU; a luminometer-dependent fraction of a photon).  相似文献   
22.
A facile synthetic route for the synthesis of bisphosphonates in phenols is described. Preparations of some of bisphosphonates, which are presently in clinical use such as risedronic acid and alendronate sodium, are synthesized following this new, simple method. This procedure can be useful for the synthesis of this class of bone‐resorptive inhibitors in bulk quantities.  相似文献   
23.
Both enantiomers of 1,2-0-isopropylidene-1,2,4-butanetriol were prepared by two different and simple methods starting from readily available L-ascorbic and D-isoascorbic acids.  相似文献   
24.
The electrical performance of stabilized lipid monolayers on H-terminated silicon is reported for the first time. We show that these 2.7 nm thick only ultrathin layers present extremely low current leakage at high electric field and high breakdown voltage that both compare favorably with the best data reported on organic thin film dielectrics. We demonstrate a very unique property of autonomic self-healing of the layer at room temperature with the total recovery of its performance after electrical breakdown. The mechanisms involved in breakdown and self-healing are described.  相似文献   
25.
Nanoparticle catalysts based on SnO2 were processed by two different methods, víz.the polymeric precursor and high-energy mechanical milling. The sample morphology and catalytic performance in the aldol condensation between methanol and acetone were modified by the processing and rare earth doping. This revised version was published online in August 2006 with corrections to the Cover Date.  相似文献   
26.
In this study, a mathematical model previously proposed for the transmission dynamics of brucellosis among bison was mathematically analyzed. Our qualitative and quantitative findings support the general hypothesis that the infection will vanish from the herd when the basic reproduction number R0<1 and will persist otherwise. A global sensitivity analysis was conducted, and the results of the Sobol indices indicated that the rate of loss of resistance (δ) and the recovery rate (v) were responsible for most of the variability in the expected number of infectious bison. On the other hand, according to the partial ranked correlation coefficients, the density‐dependent reduction in birth (φ), the mortality rate (m), the transmission coefficient (β), and the recovery rate (v) exerted very high (and negative) correlations with the number of infectious bison, whereas the rate of loss of resistance (δ) and the calving rate (a) exerted very high (and positive) correlations with the number of infectious bison. Control measures should therefore aim at increasing the magnitude of φ, m, and v and reducing those of δ and a. In addition, experimental studies are needed to precisely estimate the rate of loss of resistance and the recovery rate in order to increase the accuracy of the expected number of infectious bison. Copyright © 2014 John Wiley & Sons, Ltd.  相似文献   
27.
Development of the nanodevice that myosin-coated beads "walk" on actin filaments (F-actin) tracks for in vitro nanotransportation was hindered due to the difficulty of assembling large-area well-orientated F-actin tracks on the surface. In this work, we present a selective attachment of F-actin with controlled length on a patterned surface by employing biotinylated capped protein gelsolin as intermediate anchoring bridge. A patterned streptavidin layer was formed via coupling with a biotin layer that photo-actively attached to an amine-functionalized glass surface. The patterned film was found stable and homogenous compared to that obtained by microcontact printing method, according to the profiling with fluorescence microscopy. By a secondary blocking process, non-specific binding of F-actin to the patterned surface through electrostatic adsorption can be resisted. The length variation of F-actin as a function of gelsolin concentration was also investigated, implying that F-actin is appropriately of 2.5 μm in average length once F-actin/gelsolin molar ratio is 4:1. Finally, the selective attachment of F-actin was well characterized with quantifying the number of attached F-actin per unit area in the patterned areas over that in blocked areas. The density of F-actin was estimated at c.a. 2 μm(2) per actin filament molecule so that the distance between one another actin filament is estimated as c.a. 1.41-1.97 μm. The unique properties of F-actin, e.g. well flexibility or electrical conductivity, make it feasible to lay them down and form unidirectional aligned tracks by fluidic flow or electrical field. This may open a possibility for the long-distant movement of myosin-coated beads, offering a novel discipline for the development of micro-biochip in vitro.  相似文献   
28.
The focus of this paper was to gain a true understanding of the impact of a multifunctional epoxide (Joncryl®;ADR-4368) on the interfacial properties of biopolymer blends based on poly(lactic acid) (PLA) and poly(butylene adipate-co-terephthalate) (PBAT). The effect of Joncryl on the shear rheological, morphological, and interfacial properties of the blends was systematically investigated. For the deformed drop retraction experiments, different sandwich model systems (droplet/matrix), representing various scenarios of compatibilization, were prepared, aiming to probe the role of the epoxy-functionalized chains on the interface. The decrease of the interfacial tension in the modified/compatibilized PLA_PBAT and the formation of the PLA-Joncryl-PBAT copolymer were highlighted. A new relaxation peak relative to this copolymer was detected by the relaxation spectrum. Transient start-up shear and nonlinear stress relaxation experiments were carried out and confirmed the obtained results. In addition, the interface contribution was demonstrated using the Lee and Park model. The relaxation time increased with the amount of added Joncryl. Hence, the coexistence of chain extension/branching chains coupled to the PLA-Joncryl-PBAT copolymer formation had to be taken into account to explain the improved mechanical properties.  相似文献   
29.
Silica-based materials with hierarchical pore systems at three different length scales (small mesopores-large mesopores-macropores) have been prepared through a nanotectonic approach by using mesoporous nanoparticles as building blocks; the resulting materials present a highly accessible foam-like architecture and can be prepared as large monoliths.  相似文献   
30.
In the area of optimal design and control of queues, the N-policy has received great attention. A single server queueing system with system disaster is considered where the server waits till N customers accumulate in the queue and upon the arrival of Nth customer the server begins to serve the customers until the system becomes idle or the occurrence of disaster whichever happens earlier. The system size probabilities in transient state are obtained in closed form using generating functions and steady-state system size probabilities are derived in closed form using generating functions and continued fractions. Further, the mean and variance for the number of customers in the system are derived for both transient and steady states and these results are deduced for the specific models. Time-dependent busy period distribution is also obtained. Numerical illustrations are also shown to visualize the system effect.  相似文献   
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