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Thus synthesized thienopyrimidine derivatives were evaluated
2022-06-02
Thus synthesized thienopyrimidine derivatives were evaluated in vitro for GPR119 agonistic activity, and the results are summarized in , , . First, we fixed the 4-methylsulfonylphenyl substituent at the R position on the thienopyrimidine ring, and derivatized at the R position. As shown in , and s
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Treatment with probiotics can also be used to alter
2022-06-02
Treatment with probiotics can also be used to alter the microbiota profile of CF patients. One study reports that administration of the probiotic Lactobacillus Reuteri improved digestive health and inflammation [112]. The fecal microbial profile changed, showing a decrease in Proteobacteria and an i
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Growth hormone secretagogue receptor GHSR
2022-06-01
Growth hormone secretagogue receptor (GHSR) is a member of G-protein-coupled receptor family [3]. GHSR is predominantly expressed in human pituitary, rhypothalamus and hippocampus [4]. GHSR is also expressed in peripheral tissues including lungs, liver, kidney, and adrenal gland. In cardiovascular s
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A model substance often used in
2022-06-01
A model substance often used in the studies of oxidative processes in erythrocytes is tert-butyl hydroperoxide (t-BHP), which, being lipophilic, passes easily across the erythrocyte membrane [9]. In erythrocytes treated with t-BHP (0.1–3mM) for less than 1h, a dramatic decline in the reduced glutath
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Until recently the mechanism of how GSMs shifted secretase
2022-06-01
Until recently the mechanism of how GSMs shifted γ-secretase cleavage was poorly understood. Today, building on the sequential cleavage model developed by Ihara and colleagues [14], there is evidence that GSMs act as processivity enhancers, and iGSMs as inhibitors of processivity [120]. At least for
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In addition several other considerations were made
2022-06-01
In addition, several other considerations were made for the optimization exercise. While the structural features of the endogenous ligands for long-chain fatty BMI1 inhibitor receptors suggest obtaining orthosteric agonists with drug-like properties may be challenging, the optimization efforts were
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Through the analysis of various synthetic
2022-06-01
Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic Remodelin motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering TAK
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To explain the corporate debt
2022-06-01
To explain the corporate debt maturity, following Brockman et al. (2010), the time-varying control variables we include are: firm size (LSIZE), the square of firm size (LSIZE2), leverage (LEVERAGE), asset maturity (ASSET_MAT), managerial ownership (OWN), market-to-book ratio (MB), term structure of
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GNE-317 br Introduction Isoprenoid structures play an essent
2022-06-01
Introduction Isoprenoid structures play an essential role in biology and over 30,000 natural products of this class are known (Greenhagen et al., 2003). Like other animals, insects require these compounds for many disparate processes, including electron transport (e.g., ubiquinones), protein glyc
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The hyperacetylation of histone proteins by HATs is
2022-06-01
The hyperacetylation of histone proteins by HATs is known to be associated with gene activation [51]. In particular, p300, which is a transcription factor having HAT activity, links activators to the transcription machinery at promoters [52]. The p300/CBP complex dynamically regulates hundreds of di
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br Discussion The aim of the present study was
2022-06-01
Discussion The aim of the present study was to extend the list of ASIC ligands and to check if histamine receptors ligands can also affect ASICs. The novel finding is that not only histamine but also thioperamide, 1-metylhistamine and Nα-methylhistamine are active ASIC1a potentiators, while other
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Importantly the regulation of the Hippo
2022-06-01
Importantly, the regulation of the Hippo pathway by metabolic networks, such as by glycolysis39, 40, hexosamine biosynthesis41, 42, and mevalonate synthesis43, 44, as well as by nutrient-sensing pathways including AMP-activated protein kinase (AMPK) 40, 45, 46 and mTOR 47, 48, 49, 50, was recently d
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Pyrimethamine Hexokinases HXKs are major regulatory
2022-06-01
Hexokinases (HXKs) are major regulatory enzymes in sugar metabolism and in sugar sensing in plants (Claeyssen and Rivoal, 2007, Granot et al., 2013, Sheen, 2014, Aguilera-Alvarado and Sánchez-Nieto, 2017). HXK can phosphorylate both glucose and fructose to respective hexose-6-phosphates as a first s
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br Introduction Nicotinic acid has been
2022-05-31
Introduction Nicotinic pop over here has been used clinically for more than 50 years [1] since it has anti-atherogenic effects, including the ability to reduce triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C), and elevate high-density lipoprotein cholesterol (HDL-C) [2]. Nicotini
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Although it is currently unknown why the
2022-05-31
Although it is currently unknown why the longer splice variant found in the human has not been found in any other species, similar results have been reported for other receptors, including the Pazopanib receptor splice variant ERbeta2 identified in human and primate, but not other species (Sierens,
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