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排序方式: 共有1464条查询结果,搜索用时 31 毫秒
1.
Dr. Anders Højgaard Hansen Henriette B. Christensen Dr. Sunil K. Pandey Dr. Eugenia Sergeev Alice Valentini Julia Dunlop Domonkos Dedeo Simone Fratta Dr. Brian D. Hudson Prof. Graeme Milligan Prof. Trond Ulven Prof. Elisabeth Rexen Ulven 《ChemMedChem》2021,16(21):3326-3341
Free fatty acid receptor 2 (FFA2) is a sensor for short-chain fatty acids that has been identified as an interesting potential drug target for treatment of metabolic and inflammatory diseases. Although several ligand series are known for the receptor, there is still a need for improved compounds. One of the most potent and frequently used antagonists is the amide-substituted phenylbutanoic acid known as CATPB ( 1 ). We here report the structure-activity relationship exploration of this compound, leading to the identification of homologues with increased potency. The preferred compound 37 (TUG-1958) was found, besides improved potency, to have high solubility and favorable pharmacokinetic properties. 相似文献
2.
Matej Vizovisek Dragana Ristanovic Stefano Menghini Michael G. Christiansen Simone Schuerle 《International journal of molecular sciences》2021,22(5)
In recent decades, dysregulation of proteases and atypical proteolysis have become increasingly recognized as important hallmarks of cancer, driving community-wide efforts to explore the proteolytic landscape of oncologic disease. With more than 100 proteases currently associated with different aspects of cancer development and progression, there is a clear impetus to harness their potential in the context of oncology. Advances in the protease field have yielded technologies enabling sensitive protease detection in various settings, paving the way towards diagnostic profiling of disease-related protease activity patterns. Methods including activity-based probes and substrates, antibodies, and various nanosystems that generate reporter signals, i.e., for PET or MRI, after interaction with the target protease have shown potential for clinical translation. Nevertheless, these technologies are costly, not easily multiplexed, and require advanced imaging technologies. While the current clinical applications of protease-responsive technologies in oncologic settings are still limited, emerging technologies and protease sensors are poised to enable comprehensive exploration of the tumor proteolytic landscape as a diagnostic and therapeutic frontier. This review aims to give an overview of the most relevant classes of proteases as indicators for tumor diagnosis, current approaches to detect and monitor their activity in vivo, and associated therapeutic applications. 相似文献
3.
Fault detection and identification for a class of continuous piecewise affine systems with unknown subsystems and partitions 下载免费PDF全文
Nikolaos Moustakis Bingyu Zhou Thuan Le Quang Simone Baldi 《International Journal of Adaptive Control and Signal Processing》2018,32(7):980-993
This paper establishes a novel online fault detection and identification strategy for a class of continuous piecewise affine (PWA) systems, namely, bimodal and trimodal PWA systems. The main contributions with respect to the state‐of‐the‐art are the recursive nature of the proposed scheme and the consideration of parametric uncertainties in both partitions and in subsystems parameters. In order to handle this situation, we recast the continuous PWA into its max‐form representation and we exploit the recursive Newton‐Gauss algorithm on a suitable cost function to derive the adaptive laws to estimate online the unknown subsystem parameters, the partitions, and the loss in control authority for the PWA model. The effectiveness of the proposed methodology is verified via simulations applied to the benchmark example of a wheeled mobile robot. 相似文献
4.
Uta Klement Johanna Ekberg Simone Creci Stephen T. Kelly 《Journal of Coatings Technology and Research》2018,15(4):753-757
A large variety of coatings are used to protect structural engineering materials from corrosion, wear, and erosion, and to provide thermal insulation. In this work, yttria-stabilized zirconia coatings produced by suspension plasma spraying were investigated with respect to their microstructure and especially their porosity, as the porosity affects the thermal insulation of the underlying component. To determine porosity, pore size distribution, and pore shape, the coatings were investigated using novel advanced characterization techniques like NMR cryoporometry and X-ray microscopy. In general, the porosity is inhomogeneously distributed and the coatings showed a large variety of pore sizes ranging from a few nanometers to micrometers. 相似文献
5.
6‐Dihydroparadol,a Ginger Constituent,Enhances Cholesterol Efflux from THP‐1‐Derived Macrophages 下载免费PDF全文
Dongdong Wang Verena Hiebl Angela Ladurner Simone L. Latkolik Franz Bucar Elke H. Heiß Verena M. Dirsch Atanas G. Atanasov 《Molecular nutrition & food research》2018,62(14)
1 Scope
Ginger is reported to be used for the prevention and treatment of cardiovascular diseases (CVD). Cholesterol efflux from macrophage foam cells is an important process in reverse cholesterol transport, whose increase may help to prevent or treat CVD. In this study, we investigated the effects of 6‐dihydroparadol from ginger on macrophage cholesterol efflux.2 Methods and results
We show that 6‐dihydroparadol concentration‐dependently enhances both apolipoprotein A1‐ and human plasma–mediated cholesterol efflux from cholesterol‐loaded THP‐1‐derived macrophages using macrophage cholesterol efflux assay. 6‐Dihydroparadol increases protein levels of both ATP‐binding cassette transporters A1 and G1 (ATP‐binding cassette transporter A1 [ABCA1] and ATP‐binding cassette transporter G1 [ABCG1]) according to Western blot analysis. The ABCA1 inhibitor probucol completely abolishes 6‐dihydroparadol‐enhanced cholesterol efflux. Furthermore, increased ABCA1 protein levels in the presence of 6‐dihydroparadol were associated with both increased ABCA1 mRNA levels and increased ABCA1 protein stability. Enhanced ABCG1 protein levels were only associated with increased protein stability. Increased ABCA1 protein stability appeared to be the result of a reduced proteasomal degradation of the transporter in the presence of 6‐dihydroparadol.3 Conclusion
We identified 6‐dihydroparadol from ginger as a novel promoter of cholesterol efflux from macrophages that increases both ABCA1 and ABCG1 protein abundance. This newly identified bioactivity might contribute to the antiatherogenic effects of ginger. 相似文献6.
Enrico Casella Marco Ortolani Simone Silvestri Sajal K. Das 《Personal and Ubiquitous Computing》2020,24(4):451-464
Recognizing users’ daily life activities without disrupting their lifestyle is a key functionality to enable a broad variety of advanced services for 相似文献
7.
8.
Mina Shiran Chaharsoughi Dan Zhao Xavier Crispin Simone Fabiano Magnus P. Jonsson 《Advanced functional materials》2019,29(28)
Sensors for monitoring temperature, heat flux, and thermal radiation are essential for applications such as electronic skin. While pyroelectric and thermoelectric effects are suitable candidates as functional elements in such devices, both concepts show individual drawbacks in terms of zero equilibrium signals for pyroelectric materials and small or slow response of thermoelectric materials. Here, these drawbacks are overcome by introducing the concept of thermodiffusion‐assisted pyroelectrics, which combines and enhances the performance of pyroelectric and ionic thermoelectric materials. The presented integrated concept provides both rapid initial response upon heating and stable synergistically enhanced signals upon prolonged exposure to heat stimuli. Likewise, incorporation of plasmonic metasurfaces enables the concept to provide both rapid and stable signals for radiation‐induced heating. The performance of the concept and its working mechanism can be explained by ion–electron interactions at the interface between the pyroelectric and ionic thermoelectric materials. 相似文献
9.
Simone Grassi Oscar Campuzano Mnica Coll Francesca Cazzato Georgia Sarquella-Brugada Riccardo Rossi Vincenzo Arena Josep Brugada Ramon Brugada Antonio Oliva 《International journal of molecular sciences》2021,22(8)
Inherited cardiomyopathies are frequent causes of sudden cardiac death (SCD), especially in young patients. Despite at the autopsy they usually have distinctive microscopic and/or macroscopic diagnostic features, their phenotypes may be mild or ambiguous, possibly leading to misdiagnoses or missed diagnoses. In this review, the main differential diagnoses of hypertrophic cardiomyopathy (e.g., athlete’s heart, idiopathic left ventricular hypertrophy), arrhythmogenic cardiomyopathy (e.g., adipositas cordis, myocarditis) and dilated cardiomyopathy (e.g., acquired forms of dilated cardiomyopathy, left ventricular noncompaction) are discussed. Moreover, the diagnostic issues in SCD victims affected by phenotype-negative hypertrophic cardiomyopathy and the relationship between myocardial bridging and hypertrophic cardiomyopathy are analyzed. Finally, the applications/limits of virtopsy and post-mortem genetic testing in this field are discussed, with particular attention to the issues related to the assessment of the significance of the genetic variants. 相似文献
10.
Andrea Bedon Jean Paul Viricelle Mathilde Rieu Simone Mascotto Antonella Glisenti 《International Journal of Hydrogen Energy》2021,46(27):14735-14747
In this contribution brownmillerite-based nanocomposite cathode for Single-Chamber Solid Oxide Fuel Cells is developed. These cells can be very attractive especially for small and cheap devices because of the absence of seals. The efficiency of SC-SOFCs is strictly connected to the selectivity of anode and cathode, the bottleneck for this technology. The development of a cathode inert in fuel oxidation is particularly challenging. Our strategy is to start from a catalytically un-active support (CFA = Ca2FeAl0.95Mg0.05O5) and induce the formation of iron oxide based nanoparticles, expected to activate oxygen. Symmetric (CFA + FeOx/CGO/CFA + FeOx) and complete cells (CFA + FeOx/CGO/Ni-CGO) are studied in air and methane/oxygen 2:1 mixture. The Area Specific Resistance of CFA + FeOx is less than 1/3 that of CFA. The high selectivity allows to reach an efficiency of 25%; power still needs to be increased but we demonstrated the possibility to develop selective low cost electrodes. The effect of air, methane/oxygen exposure and the heat treatments were carefully investigated. 相似文献