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71.
72.
Yi‐Hui Peng Dr. Mohane Selvaraj Coumar Jiun‐Shyang Leou Jian‐Sung Wu Dr. Hui‐Yi Shiao Dr. Chia‐Hui Lin Dr. Wen‐Hsing Lin Tzu Wen Lien Dr. Xin Chen Dr. John T.‐A. Hsu Dr. Yu‐Sheng Chao Dr. Chien‐Fu Huang Dr. Ping‐Chiang Lyu Dr. Hsing‐Pang Hsieh Dr. Su‐Ying Wu 《ChemMedChem》2010,5(10):1707-1716
The need to develop safer and more effective antidiabetic drugs is essential owing to the growth worldwide of the diabetic population. Targeting the PPAR receptor is one strategy for the treatment of diabetes; the PPAR agonists rosiglitazone and pioglitazone are already on the market. Here we report the identification of a potent PPAR agonist, 15 , whose PPARγ activation was more than 20 times better than that of rosiglitazone. Compound 15 was designed to incorporate an indole head with a carboxylic acid group, and 4‐phenylbenzophenone tail to achieve a PPARγ EC50 of 10 nM . Compound 15 showed the most potent PPARγ agonist activity among the compounds we investigated. To gain molecular insight into the improved potency of 15 , a structural biology study and binding energy calculations were carried out. Superimposition of the X‐ray structures of 15 and agonist 10 revealed that, even though they have the same indole head part, they adopt different conformations. The head part of 15 showed stronger interactions toward PPARγ; this could be due to the presence of the novel tail part 4‐phenylbenzophenone, which could enhance the binding efficiency of 15 to PPARγ. 相似文献
73.
Polarized differential-phase laser scanning microscope 总被引:1,自引:0,他引:1
A polarized differential-phase laser scanning microscope, which combines a polarized optical heterodyne Mach-Zehnder interferometer and a differential amplifier to scan the topographic image of a surface, is proposed. In the experiment the differential amplifier, which acts as a PM-AM converter in the experiment, converting phase modulation (PM) into amplitude modulation (AM). Then a novel, to our knowledge, phase demodulator was proposed and implemented for the differential-phase laser scanning microscope. An optical grating (1800 lp/mm) was imaged. The lateral and the depth resolutions of the imaging system were 0.5 mum and 1 nm, respectively. The detection accuracy, which was limited by the reflectivity variation of the test surface, is discussed. 相似文献
74.
Over the last several decades, many Software Reliability Growth Models (SRGM) have been developed to greatly facilitate engineers and managers in tracking and measuring the growth of reliability as software is being improved. However, some research work indicates that the delayed S-shaped model may not fit the software failure data well when the testing-effort spent on fault detection is not a constant. Thus, in this paper, we first review the logistic testing-effort function that can be used to describe the amount of testing-effort spent on software testing. We describe how to incorporate the logistic testing-effort function into both exponential-type, and S-shaped software reliability models. The proposed models are also discussed under both ideal, and imperfect debugging conditions. Results from applying the proposed models to two real data sets are discussed, and compared with other traditional SRGM to show that the proposed models can give better predictions, and that the logistic testing-effort function is suitable for incorporating directly into both exponential-type, and S-shaped software reliability models 相似文献
75.
RWSNet: a semantic segmentation network based on SegNet combined with random walk for remote sensing
Jie Jiang Chengjin Lyu Yongqiang He Xuetao Hao 《International journal of remote sensing》2013,34(2):487-505
ABSTRACTSemantic segmentation methods based on deep learning considerably improve the segmentation performance of remote sensing images. However, with the extensive application of high-resolution remote sensing images, additional details introduce considerable interference to the learning process for classification, thereby diminishing the accuracy of segmentation and resulting in blurry object boundaries. To address this problem, this study designed Random-Walk-SegNet (RWSNet), a semantic segmentation network based on SegNet combined with random walk. First, SegNet is used as the basic architecture with the sliding window strategy that optimizes the network output to improve the continuity and smoothness of segmentation. Second, seed regions of the random walk are selected in accordance with the classification output of SegNet. Third, the weights of the undirected graph edge are determined by fusing the gradient of the original image and probability map of SegNet. Finally, random walk is implemented on the entire image, thus reducing edge blur and realizing high-performance semantic segmentation of remote sensing images. In comparison with mainstream and other improved methods, the proposed network has lower complexity but better performance, and the algorithm is state-of-the-art and robust. 相似文献
76.
77.
Optimal release time for software systems considering cost, testing-effort, and test efficiency 总被引:2,自引:0,他引:2
In this paper, we study the impact of software testing effort & efficiency on the modeling of software reliability, including the cost for optimal release time. This paper presents two important issues in software reliability modeling & software reliability economics: testing effort, and efficiency. First, we propose a generalized logistic testing-effort function that enjoys the advantage of relating work profile more directly to the natural flow of software development, and can be used to describe the possible testing-effort patterns. Furthermore, we incorporate the generalized logistic testing-effort function into software reliability modeling, and evaluate its fault-prediction capability through several numerical experiments based on real data. Secondly, we address the effects of new testing techniques or tools for increasing the efficiency of software testing. Based on the proposed software reliability model, we present a software cost model to reflect the effectiveness of introducing new technologies. Numerical examples & related data analyzes are presented in detail. From the experimental results, we obtain a software economic policy which provides a comprehensive analysis of software based on cost & test efficiency. Moreover, the policy can also help project managers determine when to stop testing for market release at the right time. 相似文献
78.
79.
A gauge repeatability and reproducibility (R&R) method is developed to assess the capability of a measurement system. Although gauge capability studies have received substantial attention, few studies have investigated attribute data despite their wide application in industry. The primary aim of this research is to develop a procedure, based on the generalized linear model, to evaluate the R&R of a measurement system for attribute data. To calculate repeatability of a system, the procedure integrates the iterative weighted least squares (IWLS) method and deviance analysis. The proposed procedure is applied to an inclusion measurement system to verify its adequacy to model the process capability. Copyright © 2007 John Wiley & Sons, Ltd. 相似文献
80.
Experimental studies of residence time distribution, fill factor, temperature, and melting profiles of thermoplastic resins are presented. Residence time distributions were determined as a function of throughput and screw speed. The melting of polypropylene and low density polyethylene in the entrance region was investigated. Fill factor and temperature profiles are reported. 相似文献