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As previously stated the most unexpected
2020-06-08

As previously stated, the most unexpected finding from this series of compounds was the identification of a dimethyl isoxazole side chain that gave dramatically improved binding over the parent compounds. Holding this piece of the molecule constant, a series of analogs were made to further understan
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Preparation of the pyridyl ether analogs was accomplished
2020-06-05

Preparation of the 2-pyridyl ether analogs (–) was accomplished by alkylation of alcohol with 2-bromopyridines in the presence of NaH to afford the desired pyridyl ether analogs in low to moderate yield. Preparation of the 3-pyridyl analog was carried out by conversion of alcohol to the tosylate,
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It should be noted that there are
2020-06-05

It should be noted that there are other methods, such as artificial intelligence, like Artificial Neural Networks/ANN (such as PSO-ANN, ICA-ANN), Least Square Support Vector Machine/LSSVM, etc. [10], [11], [12], [13], [14], [15], [16], [17], [18], or molecular simulations, for modeling the fluid\'s
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The absence of an observable
2020-06-05

The absence of an observable time dependence of kobs on inhibitor concentration for Zinc protoporphyrin IX 3 with AChE and compounds 1, 3 and 4 with BuChE parallels a similar absence of time dependence for some related fluoro ketones with AChE. Nair et al. found that trifluoromethyl acetophenones w
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Cholesterol homeostasis is maintained through
2020-06-05

Cholesterol homeostasis is maintained through a tight regulation between endogenous de novo synthesis, dietary absorption, utilization and excretion of bile salts. The Luzindole receptor of cholesterol from the intestine constitutes the central part of cholesterol homeostasis in the body [41]. In p
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Triflusal Enzyme mimics belong to a type
2020-06-05

Enzyme mimics belong to a type of rising catalysts which show the similar function with their corresponding natural enzymes [20], [21], [22], [23], [24], [25], [26], [27], although their structures are different from natural enzymes. In the area of prodrug activation, the widely-used enzyme mimics a
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br Materials and methods br Results and discussion br
2020-06-05

Materials and methods Results and discussion Conclusions Codon-optimized MGSK-Lys-C was expressed at a high level in an optimized expression system as inclusion bodies. The Lys-C activity reached its maximum with about 9340 nkat/Lculture under standard (chemical) refolding conditions. The r
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br Materials and methods br Results br Discussion The
2020-06-05

Materials and methods Results Discussion The incretin hormones potently stimulate insulin secretion, and it is generally assumed that this is mediated by an endocrine mechanism such that GIP and GLP-1 through the circulation reach the islet beta rxr receptor to stimulate their secretion. H
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Transcription can also be impaired by lesions in
2020-06-05

Transcription can also be impaired by lesions in the template DNA strand, which may lead to stalling of RNA polymerase (RNAP) or to transcriptional mutagenesis, thus producing mutant RNAs and proteins [[3], [4], [5], [6], [7]]. At the same time, RNAP can act as a sensor for DNA lesions, by attractin
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br STAR Methods br Acknowledgments We are grateful
2020-06-05

STAR★Methods Acknowledgments We are grateful to Matthias Mayer at ZMBH in Heidelberg for access to his CD-spectrometer and his help in data interpretation. Technical support by Wolfgang Weinig is gratefully acknowledged. This project was financially supported by the European Union as part of t
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In laboratory strains of Escherichia coli three
2020-06-05

In laboratory strains of Escherichia coli, three mechanisms of repair for alkylated bases are known. The first involves constitutively expressed Ogt and inducible Ada methyltransferases, directly removing methyl groups from O6-methylguanine (O6meG) and O4-methylthymine (O4meT) [1], [2], [3], [4]. In
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br Role of ALDH Isoenzymes in Glioma Growth
2020-06-05

Role of ALDH Isoenzymes in Glioma Growth and Invasion ALDH family genes are commonly upregulated in gliomas, indicating ALDH-dependent cell metabolism. Specific ALDH isoenzymes have been detected in high- and low-grade tumors implicated in cell proliferation, maintenance of CSC properties, invasi
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For a physiologically relevant interaction ligand and recept
2020-06-05

For a physiologically relevant interaction, ligand and receptor have to be expressed in the same place. Collagen II is found primarily in cartilage. DDR2 is expressed in proliferating chondrocytes in vivo, and its staining pattern in tibial growth plates is similar to that of collagen II. In additio
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Our results suggest that formation of DDR b clusters may
2020-06-05

Our results suggest that formation of DDR1b clusters may be important for and precede receptor phosphorylation. Indeed, while DDR1b clustering was readily detected (by YFP signal) 30 min after collagen administration, phosphorylated DDR1 species at Y513 (present in the IJXM) were evident after 4 h o
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Opiate withdrawal promotes the activation of the corticotrop
2020-06-05

Opiate withdrawal promotes the activation of the corticotropin-releasing factor (CRF) system, a major coordinator of neuroendocrine and behavioral responses to stressors. For instance, early (8–48 h) morphine withdrawal is associated with increased CRF mRNA expression in the central nucleus of the a
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