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11.
The design, synthesis, and biological evaluation of a series of epothilone analogues with novel side chains equipped with an amino group are described. Their design facilitates potential conjugation to selective drug delivery systems such as antibodies. Their synthesis proceeded efficiently via Stille coupling of a readily available vinyl iodide and heterocyclic stannanes. Cytotoxicity studies and tubulin binding assays revealed two of these analogues to be more potent than epothilones A–D and the anticancer agent ixabepilone, currently in clinical use.  相似文献   
12.
This paper examines price expectation adjustment of house buyers and sellers to rapid changes in the housing market using data from Scotland where houses are sold through ‘first-price sealed-bid’ auctions. These auctions provide more information on market signals, incentives and the behaviour of market participants than private treaty sales. This paper therefore provides a theoretical framework for analysing revealed preference data generated from these auctions. We specifically focus on the analysis of the selling to asking price difference, the ‘bid-premium’. The bid-premium is shown to be affected by expectations of future price movements, market duration and high bidding frequency. The bid-premium reflects consumer's expectations, adapting to market conditions more promptly than asking price setting behaviour and final sale prices. The volatile conditions of the recent housing market bubble are fully reflected in the bid-premium, whereas the asking and sale prices are much less prone to rapid movements.  相似文献   
13.
This paper presents the implementation of two connected component labelling algorithms on the BLITZEN massively parallel processor that was developed recently for NASA. The topology of BLITZEN is a two-dimensional mesh that can be dynamically configured to also support diagonal data transfers. It is shown that an algorithm based on Levialdi's connected component shrinking process performs much better than a straightforward algorithm for connected component labelling.  相似文献   
14.
Endothelial and epithelial barrier function is crucial for the maintenance of physiological processes. The barrier paracellular permeability depends on the composition and spatial distribution of the cell-to-cell tight junctions (TJ). Here, we provide an experimental workflow that yields several layers of physiological data in the setting of a single endothelial cell monolayer. Human umbilical vein endothelial cells were grown on Transwell filters. Transendothelial electrical resistance (TER) and 10 kDa FITC dextran flux were measured using Alanyl-Glutamine (AlaGln) as a paracellular barrier modulator. Single monolayers were immunolabelled for Zonula Occludens-1 (ZO-1) and Claudin-5 (CLDN5) and used for automated immunofluorescence imaging. Finally, the same monolayers were used for single molecule localization microscopy (SMLM) of ZO-1 and CLDN5 at the nanoscale for spatial clustering analysis. The TER increased and the paracellular dextran flux decreased after the application of AlaGln and these functional changes of the monolayer were mediated by an increase in the ZO-1 and CLDN5 abundance in the cell–cell interface. At the nanoscale level, the functional and protein abundance data were accompanied by non-random increased clustering of CLDN5. Our experimental workflow provides multiple data from a single monolayer and has wide applicability in the setting of paracellular studies in endothelia and epithelia.  相似文献   
15.
16.
The Internet of Things (IoT) is the communications paradigm that can provide the potential of ultimate communication. The IoT paradigm describes communication not only human to human (H2H) but also machine to machine (M2M) without the need of human interference. In this paper, we examine, review and present the current IoT technologies starting from the physical layer to the application and data layer. Additionally, we focus on future IoT key enabling technologies like the new fifth generation (5G) networks and Semantic Web. Finally, we present main IoT application domains like smart cities, transportation, logistics, and healthcare.  相似文献   
17.
Levels of carbon tetrachloride and tetrachloroethene were determined for the first time in Athens in the summer of 2000. The mean CCl4 and C2Cl4 concentrations were 0.060 and 0.18 ppb, respectively. CCl4 did not exhibit significant variation throughout the measurement period or with wind direction. C2Cl4 under strong eastern winds had less than half the concentrations observed during other meteorological conditions. No diurnal variation was observed for either compound.  相似文献   
18.
In the paper we present an algorithm for creating region-adjacency-graph (RAG) pyramids on TurboNet, an experimental parallel computer system. Each level of these hierarchies of irregular tessellations is generated by independent stochastic processes that adapt the structure of the pyramid to the content of the image. RAGs can be used in multiresolution image analysis to extract connected components from labeled images. The implementation of the algorithm is discussed and performance results are presented for three different communication techniques which are supported by the TurboNet's hybrid architecture. The results indicate that efficient communications are vital to good performance of the algorithm. © 1997 by John Wiley & Sons, Ltd.  相似文献   
19.
The paper presents several parallel DSP (digital signal processing) algorithms and their performance analysis, targetting a hybrid message-passing and shared-memory architecture that has been built at New Jersey Institute of Technology. The current version of our system contains eight powerful TMS320C40 processors. The algorithms are implemented on our system using message-passing only, shared-memory only, and, if possible, a combination of both of these parallel processing paradigms. Comparisons show that TurboNet's robust, hybrid architecture results in significant performance gains because of the flexibility it introduces.  相似文献   
20.
Using a formulation of the Hartree-Fock formalism with the potential morphing method in the effective mass approximation, we calculate the effective band gap of Si nanocrystals embedded in SiO2 matrix without the existence of polysilane, as a function of their diameter in the size range 1-3.5 nm. Our results are in better agreement with the experimental data, in comparison with other existing theoretical data. For diameter smaller than 2 nm our results have the same tendency with the existing theoretical results, e.g., the discrepancy between theory and experiment seems to be essential.  相似文献   
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