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Structural changes within the heteromer induced by agonist a
2020-08-13

Structural changes within the heteromer induced by agonist administration show a high level of complication. The presented results obtained in quantitative FLIM-FRET measurements with two selective ligands match the qualitative conclusions indicated by changes in the intracellular calcium level. The
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This hydrophobic biphenyl tail gave
2020-08-13

This hydrophobic biphenyl tail gave good binding affinity for human DHODH enzyme (IC OTX-015 was found to be the main metabolite in human microsomes and it was 100-fold less active against hDHODH than the ester. In an attempt to identify the specific non-covalent binding interactions which were re
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Two in vitro reports using lung fibroblasts have
2020-08-13

Two in vitro reports using lung fibroblasts have shown that cell transmigration, using transwell migration experiments, through collagen I-coated inserts is mediated by DDR2 and the DDR2-associated signaling kinases JAK2 and ERK1/2, but not DDR1 [63] and that DDR2 regulates the adhesion of fibroblas
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br Methods br Results br Discussion
2020-08-13

Methods Results Discussion MEN91507 is a potent and selective CysLT1 receptor antagonist. Guinea-pig lung membranes have been widely used for the detection and characterization of CysLT1 receptor antagonists: in this assay the high affinity (subnanomolar) binding of [3H[leukotriene D4 or [3
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Previous studies reported that combined administration of li
2020-08-13

Previous studies reported that combined administration of licorice/GL and TWHF/TP showed reduced toxicity and equal or even potentiated therapeutic efficacy when treating arthritis (YS et al., 2006, YS et al., 2008, Zhang et al., 2007). Our findings that GL reduced exposure to TP in rats confirmed t
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Pahlavanzadeh and Fakouri Baygi employed PC SAFT EoS to
2020-08-13

Pahlavanzadeh and Fakouri-Baygi [6] employed PC-SAFT EoS to predict the I-BET 151 hydrochloride of carbon dioxide by aqueous MEA solutions. They used the ideal form of Smith–Missen algorithm to calculate liquid phase concentrations. The results illustrate acceptable accuracies so that the AAD was a
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Haggar et al reported the
2020-08-13

Haggar et al. reported the synthesis of two new series of 8-(2-imino/oxo/thioxo pyrimidin-4-yl)-4-methyl-6-nitro-2-oxo-2H-chromen-7-yl benzoates 56 (X=O, S, NH) and 8-(pyrazol-3-yl)-4-methyl-6-nitro-2-oxo-2H-chromen-7-yl benzoates 57 [Y=C(O)CH3, 2,4-(NO2)2C6H3]. The 8-acetyl-4-methyl-6-nitro-2-oxo-2
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In the context of E ligase drug discovery it
2020-08-12

In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 dir
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Contrary to the profuse dopaminergic innervation of the thal
2020-08-12

Contrary to the profuse dopaminergic innervation of the thalamus found in human and non-human primates (Brown et al., 1979, Sanchez-Gonzalez et al., 2005), in rodents, the RTn is one the few thalamic nuclei that receives dopaminergic input (Anaya-Martinez et al., 2006, Garcia-Cabezas et al., 2007, G
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br Materials methods br Results br Discussion As shown
2020-08-12

Materials & methods Results Discussion As shown by qPCR analysis, Bdnf1 expression was up-regulated by approximately fifty percent after injection of RG108. A possible explanation is that the overall methylation in promoter of exon I is decreased by the compound, therefore facilitating its
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The absence of the LIG gene
2020-08-12

The absence of the LIG3 gene in yeasts has prevented the use of genetically tractable lower eukaryotes, such as Saccharomyces cerevisiae and Schizosaccharomyces pombe, as models to gain insights into the cellular functions of and interplay between the DNA ligases encoded by the LIG1, LIG3 and LIG4 g
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Classical DHFR inhibitors such as methotrexate MTX
2020-08-12

Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino Erastin residues as well as hydrophobic in
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Addition of deoxyuridine to CY cultures led
2020-08-12

Addition of deoxyuridine to CY11 cultures led to a significant decline in the amount of uracil-DNA (Fig. 5). Deoxyuridine effectively induces the deo operon and is efficiently degraded to uracil and deoxyribose 1-phosphate by the deoA gene product, thymidine phosphorylase; a minor percentage of deox
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Testosterone is inactivated through hydroxylation
2020-08-12

Testosterone is inactivated through hydroxylation and conjugation pathways [3], [4]. 6β-Hydroxylation is the main pathway among testosterone hydroxylation processes in the liver microsome. Testosterone 6β-hydroxylation is mainly catalyzed by cytochrome P450 3A (CYP3A) [5], [6], which is expressed in
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br Introduction br Literature review and hypothesis developm
2020-08-12

Introduction Literature review and adenylate cyclase development CPA exam performance-related research has been of interest to academics for the past few decades. These studies have ranged from investigating the impact of the 150-hour requirement on pass rates (Allen & Woodland, 2006) to exam
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