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91.
Eleni Papakonstantinou Dimitrios Vlachakis Trias Thireou Panayiotis G. Vlachoyiannopoulos Elias Eliopoulos 《International journal of molecular sciences》2021,22(6)
Monocarboxylate transporters (MCTs) are of great research interest for their role in cancer cell metabolism and their potential ability to transport pharmacologically relevant compounds across the membrane. Each member of the MCT family could potentially provide novel therapeutic approaches to various diseases. The major differences among MCTs are related to each of their specific metabolic roles, their relative substrate and inhibitor affinities, the regulation of their expression, their intracellular localization, and their tissue distribution. MCT4 is the main mediator for the efflux of L-lactate produced in the cell. Thus, MCT4 maintains the glycolytic phenotype of the cancer cell by supplying the molecular resources for tumor cell proliferation and promotes the acidification of the extracellular microenvironment from the co-transport of protons. A promising therapeutic strategy in anti-cancer drug design is the selective inhibition of MCT4 for the glycolytic suppression of solid tumors. A small number of studies indicate molecules for dual inhibition of MCT1 and MCT4; however, no selective inhibitor with high-affinity for MCT4 has been identified. In this study, we attempt to approach the structural characteristics of MCT4 through an in silico pipeline for molecular modelling and pharmacophore elucidation towards the identification of specific inhibitors as a novel anti-cancer strategy. 相似文献
92.
Anita Romanowska Katarzyna Wgrzyn Katarzyna Bury Emilia Sikorska Aleksandra Gnatek Agnieszka Piwkowska Igor Konieczny Adam Lesner Magdalena Wysocka 《International journal of molecular sciences》2021,22(5)
The present study aimed to synthesize novel polycationic polymers composed of N-substituted L-2,3-diaminopropionic acid residues (DAPEGs) and investigate their cell permeability, cytotoxicity, and DNA-binding ability. The most efficient cell membrane-penetrating compounds (O2Oc-Dap(GO2)n-O2Oc-NH2, where n = 4, 6, and 8) showed dsDNA binding with a binding constant in the micromolar range (0.3, 3.4, and 0.19 µM, respectively) and were not cytotoxic to HB2 and MDA-MB-231 cells. Selected compounds used in the transfection of a GFP plasmid showed high transfection efficacy and minimal cytotoxicity. Their interaction with plasmid DNA and the increasing length of the main chain of tested compounds strongly influenced the organization and shape of the flower-like nanostructures formed, which were unique for 5/6-FAM-O2Oc-[Dap(GO2)]8-O2Oc-NH2 and typical for large proteins. 相似文献
93.
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96.
D. Thoenes 《Chemical engineering science》1980,35(9):1840-1853
Modelling of chemical reactors is reviewed with an emphasis on process development and scale-up. A distinction is made between modelling of chemical kinetics, of rate processes in volume elements and of whole reactors. Examples are mainly taken from papers presented at the Sixth International Symposium on Chemical Reaction Engineering. Special attention is given to the modelling of single phase reactors, fixed beds, trickle beds, fluid beds, and gas bubble reactors. 相似文献
97.
Jose Gerde Connie Hardy Walter Fehr Pamela J. White 《Journal of the American Oil Chemists' Society》2007,84(6):557-563
Two extruded-expelled physically refined soybean oils with reduced contents of linolenic acid, ultra-low- linolenic acid (ULL,
1.5%) and low-linolenic acid (LL, 2.6%), and a extruded-expelled physically refined control oil (control, 5.3% linolenic acid)
were evaluated by frying French fries in a commercial-like setting for 6 h day−1 during 23 days. The oils became darker, increased in yellow color at the beginning, and became redder and less green throughout
the process. Free fatty acids levels were not different among the oils until day 14, after which, ULL was different from the
control for the remainder of frying. The conjugated dienoic acid values were greatest in the control. Generally, ULL and LL
oils had lower percentages of polar compounds than did the control, providing a frying life 2 days longer than the control
and ~30% increase in frying time. A trained sensory panel evaluated the French fries on days 2, 5, and 6. Buttery and potato
flavors decreased, and rancid and painty flavors increased over frying time for all products. Rancid flavor was highest in
the fries from the control oil. Overall, the ULL and LL oils performed better than did the control oil and ULL tended to perform
better than the LL. 相似文献
98.
《International Journal of Industrial Ergonomics》2014,44(5):747-752
The purpose of this study is to validate an analytical method in assessing demanded mental workloads for physical therapists, and to discuss its possible ergonomics implications on the design of healthcare working systems in which physical therapists are considered as the users. A task analysis was first used to understand the operation steps of three identified physical therapies. Then, the McCracken–Aldrich technique was applied to assign ratings of mental workload demanded for performing each step of the therapies. Finally, the assigned ratings were validated by the analysis of correlation with the answers of the NASA-TLX questionnaire collected from seventeen physical therapists in the rehabilitation center of a university-affiliated hospital. Results showed that the proposed McCracken–Aldrich technique was suitable as an analysis tool for predicting metal workloads of physical therapists. Some possible implications about the information provision and user interface design for reducing therapists' mental workloads on current therapy operations were discussed.Relevance to industryResults of this paper are expected to contribute the research and development in healthcare industry on its system design and workflow analysis. 相似文献
100.
This paper deals with internal challenges that the human factors/ergonomics (HFE) research faces when wishing to strengthen its contribution to development of work systems. Three established characteristics of high-quality HFE, i.e., HFE takes a systems approach, HFE is design-driven, and HFE focuses on two closely related outcomes, performance and well-being, are taken as a starting point of a methodological discussion, in which conceptual innovations, e.g. adopting the technology-in-use perspective, are proposed to support development of HFE towards the high-quality aims. The feasibility of the proposed conceptual choices is demonstrated by introducing a naturalistic HFE analysis approach including four HFE functions. The gained experience of the use of this approach in a number of complex work domains allows the conclusion that becoming design-driven appears as that most difficult quality target for HFE to reach. Creating an own design discipline identity in a multi-voiced collaboration is the key internal challenge for human factors/ergonomics. 相似文献