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1.
Dr. Jelena Melesina Conrad V. Simoben Lucas Praetorius Emre F. Bülbül Dr. Dina Robaa Prof. Dr. Wolfgang Sippl 《ChemMedChem》2021,16(9):1336-1359
This review classifies drug-design strategies successfully implemented in the development of histone deacetylase (HDAC) inhibitors, which have many applications including cancer treatment. Our focus is on especially demanded selective HDAC inhibitors and their structure-activity relationships in relation to corresponding protein structures. The main part of the paper is divided into six subsections each narrating how optimization of one of six structural features can influence inhibitor selectivity. It starts with the impact of the zinc binding group on selectivity, continues with the optimization of the linker placed in the substrate binding tunnel as well as the adjustment of the cap group interacting with the surface of the protein, and ends with the addition of groups targeting class-specific sub-pockets: the side-pocket-, lower-pocket- and foot-pocket-targeting groups. The review is rounded off with a conclusion and an outlook on the future of HDAC inhibitor design. 相似文献
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Carrara Gabriel R. Burle Leonardo M. Medeiros Dianne S. V. de Albuquerque Célio Vinicius N. Mattos Diogo M. F. 《电信纪事》2020,75(3-4):163-174
Annals of Telecommunications - Blockchain is a disruptive technology that relies on the distributed nature of the peer-to-peer network while performing an agreement, or consensus, a mechanism to... 相似文献
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Changes of the cell surface hydrophobicity of Lactobacillus acidophilus La‐5 in response to pH,temperature and inulin 下载免费PDF全文
Antonio Bevilacqua Leonardo Petruzzi Barbara Speranza Daniela Campaniello Milena Sinigaglia Maria Rosaria Corbo 《International Journal of Food Science & Technology》2018,53(5):1262-1268
The main topic of this study was to study how cell surface hydrophobicity (CSH) could change in response to pH, temperature and inulin; Lactobacillus acidophilus La‐5 was used as a model microorganism. pH, temperature, inulin and incubation time (exposure to prebiotic or incubation at pH 4.0 and 9.0) were combined through a full factorial design and a Central Composite Design; the results were analysed using a multifactorial anova (first step) and a stepwise regression (second step). Temperature and pH significantly affected CSH: an increase in the temperature determined a significant increase in CSH, whereas the correlation pH vs. CSH was negative, as an increase in pH caused a significant decrease in CSH. Inulin played a significant role, but its effect could be influenced by temperature, pH and exposure time. This study is the first approach on the effects of some environmental factors on CSH and suggests that the culturing conditions and/or the exposure to some prebiotics could modify it with positive or negative effects. 相似文献
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Polyana Alves Radi Angela Vieira Lucas Manfroi Karina Carvalho de Farias Nass Marco Antonio Ramirez Ramos Priscila Leite Gislene Valdete Martins Jorge Benedito Freire Jofre Lucia Vieira 《Ceramics International》2019,45(7):9686-9693
There has been a recent increase in both the production and consumption of ethanol due to the numerous environmental advantages that it offers, such as the fact that it can be produced from a variety of renewable materials, for instance corn and cellulose, or it can be obtained from sugarcane bagasse and biomass (2nd and 3rd generation ethanol). The result of this is that nowadays ethanol is widely seen as the dominant biofuel – or as a blend component in gasoline or pure fuel - in many countries.However, one disadvantage of the use of ethanol is the high corrosive behavior that occurs when its hygroscopic properties are exposed to a large number of materials. Xiaoyuan Lou and Preet Singh showed that the increase of water concentration in ethanol induces pitting and metal loss. Diamond-Like Carbon (DLC) films may be a solution to this problem due to the fact that they can be deposited inside tubes, offer good protection levels against corrosion, and reduce the friction coefficient and wear.This paper shows the tribocorrosion and corrosion studies of DLC films deposited on stainless steel grade 304 (SS304) substrates in order to gauge its appropriateness usage in the construction of pipelines and fuel storage tanks. The surface morphology was analyzed before and after 14 days of immersion. The tribocorrosion, friction coefficient, and wear rate were studied in ethanol to see the effects of water concentration. The films showed good adherence to the substrates. Corrosion and tribocorrosion results showed that for bare Stainless Steel 304 the increase of the water content increases the corrosion and the friction coefficient. DLC coated samples presented few points of delamination, and the friction coefficient and open circuit potentials were very low compared with the bare sample which was water concentration independent. 相似文献
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Miccoli Leonardo Agatino 《电源世界》2019,(2)
车内系统的电子产品含量持续成长,原因是市场对自动化、安全性、能耗优化和高质量体验的要求越来越高。在此背景之下,使用直流马达的应用数量也不断上扬。 相似文献
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Luca Pezzato Leonardo Bertolucci Coelho Rachele Bertolini Alessio Giorgio Settimi Katya Brunelli Marjorie Olivier Manuele Dabal 《工业材料与腐蚀》2019,70(11):2103-2112
Plasma electrolytic oxidation (PEO) coatings were produced on AZ80 magnesium alloy in a solution containing silicates and phosphates and working at high current densities with short treatment times. The effect of a sealing treatment in boiling water on corrosion and mechanical properties of the coatings were investigated. Moreover, the corrosion mechanism of the samples with and without the sealing treatment was evaluated. The microstructure of the coatings was characterized with scanning electron microscope observation and X‐ray diffraction analysis. The mechanical properties were evaluated with nanoindentation tests and the corrosion resistance was studied by potentiodynamic polarization, electrochemical impedance spectroscopy, and scanning vibrating electrode technique. The results showed that the sealing did not influence the microstructure and the mechanical properties of the samples and instead produced a remarkable increase in the corrosion resistance. The crevice corrosion, present in the sample without the sealing, was avoided with the treatment in boiling water. 相似文献
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Deborah Oliveira De Fusco Leonardo Lucas Madaleno Vanildo Luiz Del Bianchi Aline da Silva Bernardo Rafael Roberto Assis Gustavo Henrique de Almeida Teixeira 《International Journal of Food Science & Technology》2019,54(7):2416-2424
Alcohol-free beer with isotonic properties is getting more popular and its production can be carried out by different production strategies; however, interrupted fermentation is still a challenge. Therefore, the objective of this study was to develop a low-alcohol isotonic beer (<0.5% v/v) by interrupted fermentation. Moreover, the major objective is to compare the developed product to commercial beverages (sports drinks, ‘Pilsen' regular beer, alcohol-free beers and low-alcohol isotonic beer). The beverages were evaluated based on pH, alcohol content (% v/v), total titratable acidity (mEq L−1), osmolality (mOsmol kg−1), bitterness International Bitterness Units, colour European Brewery Convention, total phenolic compounds (mg L−1 gallic acid), reducing and total sugars (%) and Na and K contents (mg L−1). The developed low-alcohol isotonic beer presented characteristics similar to sports drinks, with the advantage of being richer in phenolic compounds and suitable osmolality. Despite salts were added in its formulation, the grades attributed to all beers employed in the sensory evaluation, as well as the purchase intention did not present significant differences. 相似文献