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72.
Akihiro Honda Shotaro Kamata Makoto Akahane Yui Machida Kie Uchii Yui Shiiyama Yuki Habu Saeka Miyawaki Chihiro Kaneko Takuji Oyama Isao Ishii 《International journal of molecular sciences》2022,23(9)
Among the agonists against three peroxisome proliferator-activated receptor (PPAR) subtypes, those against PPARα (fibrates) and PPARγ (glitazones) are currently used to treat dyslipidemia and type 2 diabetes, respectively, whereas PPARδ agonists are expected to be the next-generation metabolic disease drug. In addition, some dual/pan PPAR agonists are currently being investigated via clinical trials as one of the first curative drugs against nonalcoholic fatty liver disease (NAFLD). Because PPARα/δ/γ share considerable amino acid identity and three-dimensional structures, especially in ligand-binding domains (LBDs), clinically approved fibrates, such as bezafibrate, fenofibric acid, and pemafibrate, could also act on PPARδ/γ when used as anti-NAFLD drugs. Therefore, this study examined their PPARα/δ/γ selectivity using three independent assays—a dual luciferase-based GAL4 transactivation assay for COS-7 cells, time-resolved fluorescence resonance energy transfer-based coactivator recruitment assay, and circular dichroism spectroscopy-based thermostability assay. Although the efficacy and efficiency highly varied between agonists, assay types, and PPAR subtypes, the three fibrates, except fenofibric acid that did not affect PPARδ-mediated transactivation and coactivator recruitment, activated all PPAR subtypes in those assays. Furthermore, we aimed to obtain cocrystal structures of PPARδ/γ-LBD and the three fibrates via X-ray diffraction and versatile crystallization methods, which we recently used to obtain 34 structures of PPARα-LBD cocrystallized with 17 ligands, including the fibrates. We herein reveal five novel high-resolution structures of PPARδ/γ–bezafibrate, PPARγ–fenofibric acid, and PPARδ/γ–pemafibrate, thereby providing the molecular basis for their application beyond dyslipidemia treatment. 相似文献
73.
74.
基于支持向量机的中文娱乐新闻词语的识别 总被引:1,自引:0,他引:1
在应用基本的支持向量机算法的基础上,提出了一种新的分布增量学习方法,利用主动学习策略对训练样本进行选择,逐步增大提交给学习器训练样本的规模,以提高学习器的识别精确率.实验表明,采用主动学习策略的支持向量机算法是有效的,中文娱乐新闻词语识别的正确率和召回率分别达到了78.92%和86.42%,收到了良好的效果. 相似文献
75.
我国经济的不断发展为各个行业均带来了机遇,尤其是第三产业,随着社会经济的发展和人民消费需求的提高,娱乐业发展迅速,公共娱乐场所不断增多,遍布城市每个角落,规模也在不断扩大,满足了人们的精神生活需求。然而随之带来的安全隐患,尤其是火灾隐患,使其成为消防部门重点监管对象。公共娱乐场所内人员较多和装修材料复杂,其中一些营业面积较大,一旦发生火灾,难以在第一时间通知到场所内的所有人员并进行快速疏散,在火灾威胁下,极易造成群死群伤等重大事故。 相似文献
76.
随着我国市场经济的不断发展以及人们物质生活水平的提高,公共娱乐场所逐渐成为人们休闲娱乐的地方。文章重点阐述了公共娱乐场所注重防火的意义以及发生火灾的特点,并对其存在的火灾隐患及防火对策做出了分析,旨在倡导大家关注公共消防安全,营造美好幸福生活。 相似文献
77.
A computer simulation model of salt pan is presented. The transient behavior and the effects of various parameters of the salt pans, such as the depth of the brine layer, the absorptance of the soil surface, the thermal properties of the soil beneath the brine layer and the depth of the underground water table, on the evaporation process of salt pans are discussed. The effects of extra insulation layer and the intensity of solar radiation are also examined. 相似文献
78.
Fine polyamide 66 (PA66) powder was prepared in a shear pan mill that was designed and developed in our laboratories. In contrast with discontinuous impacts in the ball mill, the size reduction operation in the pan mill is characterized by application of uninterrupted strong shear forces on particles. It has been found that as compared to the ball mill, much finer pulverization of the polymer material is achieved in the pan mill, in spite of the high strength and ductility of the polymer. Sodium sulfate ionic crystals with hard and pointed edge were co-milled with PA66 to further cut the fine polymer particles into ultrafine powder (2–5?µm). Besides acting as a grinding aid, the ionic crystals also prevented conglutination and aggregation of the polymer powder. Furthermore, PA66 powder could be conveniently separated and purified from the co-milled grinding aid-polymer mixture by simple water washing and filtration. Thus, an energy efficient and environment-friendly technology has been developed to prepare the ultrafine plastic powder at room temperature. This process holds a good promise for commercial applications. 相似文献
79.
George Boskou Fotini N. Salta Antonia Chiou Elena Troullidou Nikolaos K. Andrikopoulos 《European Journal of Lipid Science and Technology》2006,108(2):109-115
Trans,trans‐2,4‐decadienal is a by‐product of frying oil that is also transferred to fried food. This aldehyde has been found and quantified both in frying oils and fumes generated during frying. Furthermore, it has been reported that 2,4‐decadienal has cytotoxic and genotoxic effects and promotes LDL oxidation. In the present work trans,trans‐2,4‐decadienal was detected directly in fried potatoes (french‐fries). Moreover, the influence of frying conditions (deep‐frying, pan‐frying), the oil type (olive oil, sunflower oil, cottonseed oil, palm oil and a vegetable shortening) and the degree of thermal deterioration (eight successive frying sessions without replenishment) on the production of 2,4‐decadienal in oil and potatoes was studied. The isolation of the aldehyde was performed by methanol extraction, while the identification and quantification was performed by RP‐HPLC. The quantity of trans,trans‐2,4‐decadienal produced during successive pan‐frying demonstrated a peak at the third and fourth frying session. The highest concentration of trans,trans‐2,4‐decadienal was detected in potatoes fried in sunflower oil, and the lowest in olive oil. The quantity of trans,trans‐2,4‐decadienal in fried potatoes decreased during successive deep‐frying at the seventh frying session or remained stable, except for cottonseed oil. The quantity of trans,trans‐2,4‐decadienal in fried potatoes was considered to be dependent on the oil used, on the frying process and, to a lesser extent, on the oil deterioration. In all cases tested, the highest concentration of trans,trans‐2,4‐decadienal was detected during deep‐frying. The unsaturation degree of the frying oil was considered to promote the formation of trans,trans‐2,4‐decadienal. Considering the quantity of 2,4‐decadienal found in french‐fries and in the respective frying medium, direct quantification of 2,4‐decadienal is required in order to make an estimation of intake from french‐fries. 相似文献
80.
路况PTZ摄像机自动标定方法 总被引:2,自引:0,他引:2
李勃 《北京邮电大学学报》2009,32(21):24-29
为解决路况pan/tilt/zoom(PTZ)摄像机内外参数实时多变,绝对距离难以求解的问题,提出了一种基于路况图像的自动化标定方法: 建立全新的路况PTZ摄像机成像模型; 根据图像中提取的路面点的相对距离关系,推导模型中各未知参数的求解方法,实现摄像机参数的“白盒”标定,并给出了自动化标定的实现方案; 摘录实际路况试验结果,计算标定误差. 该算法只需要路面场景图像即可实现自动标定,无须人为干涉和配置,其计算简单,灵活性好,非常符合智能交通监控系统的需求. 相似文献