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We hypothesize that both IGF dependent kinase
2021-01-22

We hypothesize that both IGF-1-dependent kinase activation and locally synthesized neuroestrogens interactively regulate estrogen receptor activity in neuronal biotin-LC-LC-tyramide in the absence of exogenously applied estradiol. The Neuro-2A cell line was chosen as the model system for these stud
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Fesoterodine Fumarate br Abbreviations br Introduction br Co
2021-01-22

Abbreviations Introduction Collagen-induced DDR activation A key feature of DDRs is their ability to bind both fibrillar and non-fibrillar collagens (Shrivastava et al., 1997, Vogel et al., 1997). DDR1 and DDR2 recognize the GVMGVO (O, hydroxyproline) motif within fibrillar collagens I–III
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Following DEX exposure the levels of CYP A protein and
2021-01-22

Following DEX exposure, the levels of CYP1A1 protein and activity remained unchanged, as seen in our previous in vitro study (Burkina et al., 2013). Dasmahapatra and Lee (1993) reported that 3.9μgL−1 DEX, similar to our highest tested concentration, did not change CYP1A1 protein content. An increase
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Oxysterols modulate the immune responses and as such could
2021-01-22

Oxysterols modulate the immune responses and as such could be effectors of the tumor environment: 25-OHC impairs IgA production in B-lymphocytes [26] and induces the secretion of the proinflammatory and angiogenic cytokine IL-8 [27], [28]. Of note, oxysterols (in particular 7α,25-OHC) are potent che
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Because EBI is expressed on the major subsets of immune
2021-01-22

Because EBI2 is expressed on the major subsets of immune cells, and small molecule antagonists for EBI2 were recently described (Benned-Jensen et al., 2013, Gessier et al., 2014), EBI2 constitutes a tempting drug target reminiscent of the sphingosine-1-phosphate receptor superagonist fingolimod/Gile
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Mono and bi ubiquitination of
2021-01-22

Mono- and bi-ubiquitination of two lysines, namely K70 and K76, in a small fraction of p33 replication co-factor has been demonstrated in yeast (Barajas and Nagy, 2010, Li et al., 2008). Because mutations of these lysines reduced TBSV repRNA replication in yeast and affected the ability of p33 to in
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Although many GPCR heteromers have been identified
2021-01-22

Although many GPCR heteromers have been identified using heterologous cell lines, only very few fit all three criteria. This is mainly due to the difficulties to study these structures in native tissues because of the lack of sensitive and selective tools, not only capable of detecting in vivo evide
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We recently reported that the information about the
2021-01-21

We recently reported that the information about the electronic density obtained from a QTAIM analysis is useful to describe the molecular interactions that stabilize and destabilize the different complexes L-R [13], [14], [15]. Specifically in our previous work reported for DHFR inhibitors, the QTAI
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We found that both DDR and DDR ECD
2021-01-21

We found that both DDR1 and DDR2 ECD increased matrix mineralization as compared to native cells, with the effect of DDR2 ECD being more prominent. Both soluble (DDR2/ECD) and membrane-bound DDR2 ECD (DDR2/-KD), when compared to wild-type cells, induced larger mineral deposits. In this regard, a rec
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In recent years the use of liquid chromatography
2021-01-21

In recent years, the use of liquid chromatography/tandem mass spectrometry (LC–MS/MS) has become a preferred approach to measure drugs and metabolites in biological fluids due to its very high selectivity and sensitivity [17], [18], [19], [20], [21], [22], [23], [25], [30]. The great sensitivity of
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The CYP A genes are regulated physiologically by glucocortic
2021-01-21

The CYP3A genes are regulated physiologically by glucocorticosteroids, growth hormone, thyroid hormones and cytokines [13, 20, 30]. It has been shown that glucocorticoid receptor (GR), pregnane X receptor (PXR), constitutive androstane receptor (CAR) and vitamin D receptor (VDR) play an important ro
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Our results for imidacloprid were unexpected considering tha
2021-01-21

Our results for imidacloprid were unexpected: considering that imidacloprid (Im) is a neonicotinoid insecticide with a different mode of action (agonist of the nicotinic Furosemide receptor) than OPs, we expected Es-ChE and T-ChE activity to be largely insensitive to changes in Im concentrations. Ho
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Propranolol initially discovered in is
2021-01-21

Propranolol, initially discovered in 1964, is first and most widely studied as a non-selective beta-blocker. Propranolol through β-adrenergic receptor blockade has reduced heart rate and blood pressure and have anti-arrhythmogenic and anti-ischemic effects, and been proposed as an effective strategy
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1-NM-PP1 synthesis Given that dimethylamine substitution was
2021-01-21

Given that dimethylamine substitution was tolerated as in SR106447 (), we investigated 1-NM-PP1 synthesis amine substitutions as replacements for the -butyl group (). Cyclic amines (SR19880, 19882) or simple mono-substituted anilines (SR20037) were not active, nor was an acetylated version (SR20039
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We next turned our attention
2021-01-21

We next turned our attention to the 6-position of the indole (). It was found that the chlorine atom present in was extremely important. The des-chloro analogue showed nearly 30-fold less affinity for the EP receptor in the binding assay and was nearly 30-fold lower in activity in the functional a
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