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101.
The design and synthesis of ethyl 4-(6-amino-7-cyano-2,3-dihydro-1H-pyrrolizine-5-carboxamido)-benzoate (KH16) were discussed, and its structure was determined. The anti-inflammatory activity of a new compound was evaluated using in vitro cyclooxygenase (COX) inhibitory assay. KH16 exhibits higher selectivity to COX-2 than to COX-1 with the selectivity index of 3.46. KH16 was labeled with 99mTc with the maximum radiochemical yield of 99mTc-KH16 of 90.5 ± 1.5%. Biodistribution of 99mTc-KH16 in normal, infected, and inflamed mice was studied. The uptake in inflamed muscle was higher than that in normal muscle throughout the examined time interval. This work is a step ahead in the direction of using pyrrolizine derivatives for site-specific delivery to the inflamed tissue. 相似文献
102.
Poonam Vishwakarma Akhila Melarkode Vattekatte Nicolas Shinada Julien Diharce Carla Martins Frdric Cadet Fabrice Gardebien Catherine Etchebest Aravindan Arun Nadaradjane Alexandre G. de Brevern 《International journal of molecular sciences》2022,23(7)
VHH, i.e., VH domains of camelid single-chain antibodies, are very promising therapeutic agents due to their significant physicochemical advantages compared to classical mammalian antibodies. The number of experimentally solved VHH structures has significantly improved recently, which is of great help, because it offers the ability to directly work on 3D structures to humanise or improve them. Unfortunately, most VHHs do not have 3D structures. Thus, it is essential to find alternative ways to get structural information. The methods of structure prediction from the primary amino acid sequence appear essential to bypass this limitation. This review presents the most extensive overview of structure prediction methods applied for the 3D modelling of a given VHH sequence (a total of 21). Besides the historical overview, it aims at showing how model software programs have been shaping the structural predictions of VHHs. A brief explanation of each methodology is supplied, and pertinent examples of their usage are provided. Finally, we present a structure prediction case study of a recently solved VHH structure. According to some recent studies and the present analysis, AlphaFold 2 and NanoNet appear to be the best tools to predict a structural model of VHH from its sequence. 相似文献
103.
Taha Ali El-Taweel S. A. Gouda 《The International Journal of Advanced Manufacturing Technology》2011,53(1-4):181-190
Electrochemical machining (ECM) has become one of the most widely spread techniques of the non-traditional processes. The main problem of ECM is that of choosing the correct working parameters to attain a high degree of accuracy under fine surface finish conditions. Recently, electrochemical turning has gained attention as a finishing process. By feeding a shaped tool into a rotating workpiece, axially symmetric turned parts can be manufactured. In this way, large symmetric workpiece can be made with small tools. This paper discusses the feasibility of using a wire as a tool in electrochemical turning process (WECT). The present study measures the performance criteria of the WECT process through investigating the effect of working parameters, namely, applied voltage, wire feed rate, wire diameter, workpiece rotational speed, and overlap distance, on metal removal rate, surface roughness, and roundness error. The experimental results are statistically analyzed and modeled through response surface methodology. The regression model adequacies are checked using analysis of variance. Furthermore, the optimal combination of these parameters has been evaluated to maximize metal removal rate and minimize surface roughness and roundness error. The study reveals the ability of using a wire as a tool in WECT and its productivity; the shape errors can be controlled through the mentioned input parameters. The results show that the increase of wire feed rate enhances the productivity of the process and improves both surface quality and roundness error. Also, the increase of rotational speed improves both the productivity of the process and geometrical error of the produced parts. 相似文献
104.
Akhila Melarkode Vattekatte Frdric Cadet Jean-Christophe Gelly Alexandre G. de Brevern 《International journal of molecular sciences》2021,22(18)
In the particular case of the Camelidae family, immunoglobulin proteins have evolved into a unique and more simplified architecture with only heavy chains. The variable domains of these chains, named VHHs, have a number of Complementary Determining Regions (CDRs) reduced by half, and can function as single domains making them good candidates for molecular tools. 3D structure prediction of these domains is a beneficial and advantageous step to advance their developability as molecular tools. Nonetheless, the conformations of CDRs loops in these domains remain difficult to predict due to their higher conformational diversity. In addition to CDRs loop diversity, our earlier study has established that Framework Regions (FRs) are also not entirely conformationally conserved which establishes a need for more rigorous analyses of these regions that could assist in template selection. In the current study, VHHs models using different template selection strategies for comparative modeling using Modeller have been extensively assessed. This study analyses the conformational changes in both CDRs and FRs using an original strategy of conformational discretization based on a structural alphabet. Conformational sampling in selected cases is precisely reported. Some interesting outcomes of the structural analyses of models also draw attention towards the distinct difficulty in 3D structure prediction of VHH domains. 相似文献
105.
The dynamic leaching of lanthanides from a west desert phosphate ore, Egypt (Abu Tartur) by hydrochloric acid, nitric acid and sulfuric acid solutions was investigated in this study as a function of acid concentration, flow rate and the presence of some additives such as boric acid. Also the kinetics of leaching of lanthanides was investigated as a function of temperature. It was found that the leaching process could be described by a shrinking-core model, with activation energy about 5.9, 13.8 and 21.9 kJ/... 相似文献
106.
107.
Anionic cotton dyeings with anti‐ultraviolet and antibacterial functions were prepared by the post‐treatment of direct and reactive cotton dyeings with a zirconium oxychloride salt solution. The extent of improvement in the functional properties was governed by the structure and pretreatment history of the knitted cotton fabric, the kind and concentration of the anionic dye, and the dyeing regime. The chelation and fixation of the positively charged zirconium ions onto and/or within the dyed substrate resulted in an enhancement in the ultraviolet absorption capacity of the treated substrate and interaction with the thiol groups of the cellular protein; this imparted antibacterial activity against Gram‐positive and Gram‐negative bacteria without adverse effects on the hue of the obtained dyeings. Both the anti‐ultraviolet and bacterial functions of the post‐treated dyeings survived through 15 washing cycles. © 2009 Wiley Periodicals, Inc. J Appl Polym Sci, 2010 相似文献
108.
Khaled Saad Mekheimer Mohamed Obeid Mohamed El-Sayed Noreen Sher Akbar Ashraf A. Gouda 《亚洲传热研究》2024,53(4):1749-1769
Thermal enhancement remains a critical requirement in different engineering applications. Many factors can affect the efficiency of the techniques used for this aim. The purpose of this study is to investigate the impact of particle-fluid suspensions with heat transfer through porous annular-sector duct on enhancement techniques and address the potential application of deep learning to suspension problems. The analysis is focused on the fully developed region of the forced convection flow. Thermal and rheological properties of particle-fluid suspensions were studied using physics-informed neural networks exploiting transfer learning capabilities for making parameter analysis. Another finite element solution was introduced as a measure of accuracy and to support our findings. Results were prepared in a comparative manner for both solvers including contour plots, tabular, and two dimensional figures. The average Nusselt number and friction factors were calculated for different cases to investigate the value of the thermal performance factor. Our results indicate the downside of suspensions on thermal enhancement and their negative impact on other techniques. 相似文献
109.
1-IntroductionPittingcorrosionisthemostdestructiveformamongthedifferentformsoflocalizedcorrosionofmetals.Thebreakdownofthepassivefilmbyag-gressiveionssuchaschlorideionscanleadtohighpenetrationrates.Copper-nickelalloysarewidelyusedascorrosionresistantmaterialsinmarineengineering.Theircor-rosionratesdecreasesharplywithincresingNicon-tent.AseriesofCu-Nialloyshavebeenwidely.tudi.d[1~12]innaturalseawaterandinNaClsolu-tionsusingdifferentelectrochemicalmethods.Con-tradictoryresultshavebeenobtained… 相似文献
110.
Arora A. Gouda M. 《IEEE transactions on pattern analysis and machine intelligence》1993,19(11):1015-1027
The authors formally define what it means for a system to tolerate a class of faults. The definition consists of two conditions. The first is that if a fault occurs when the system state is within the set of legal states, the resulting state is within some larger set and, if faults continue to occur, the system state remains within that larger set (closure). The second is that if faults stop occurring, the system eventually reaches a state within the legal set (convergence). The applicability of the definition for specifying and verifying the fault-tolerance properties of a variety of digital and computer systems is demonstrated. Using the definition, the authors obtain a simple classification of fault-tolerant systems. Methods for the systematic design of such systems are discussed 相似文献