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One of the most common
2022-03-15
One of the most common dietary approaches against obesity-associated diseases is the increase in the consumption of ω3 polyunsaturated fatty acids [18], [19]. Since seminal paper by Bang and Dyeberg in which the low prevalence of coronary heart disease among the Inuit was associated with the high ma
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Both GPR A and GPR are located on chromosome
2022-03-15
Both GPR109A and GPR81 are located on chromosome 12q24 [3] and mediate anti-lipolytic effects through coupling to Gi-type G proteins [17]. It is important to note that with the recent deorphanization of these receptors, there has been a recommendation to the International Union of Basic and Clinical
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In parallel we were also preparing
2022-03-15
In parallel, we were also preparing and evaluating other piperidine bioisosteres and modifications to – to further access additional novel intellectual property (IP) space. Modeling work suggested that 4-position homologated piperidines, as well as 3-position homologated azetidines overlapped favora
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In conclusion we have designed and characterized a
2022-03-14
In conclusion, we have designed and characterized a novel series of EAAT-blockers, exemplified by (-[4-(2-bromo-4,5-difluorophenoxy)phenyl]--asparagine)—a potent, selective, competitive non-substrate inhibitor of EAAT-2. As one of the most potent and selective EAAT-2 inhibitors identified to date,
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The Hedgehog Hh pathway is linked
2022-03-14
The Hedgehog (Hh) pathway is linked to the development of several types of epithelial cancers (Rubin and de Sauvage, 2006). A paracrine mechanism has been implicated in CAF activation, with Hh ligands secreted by cancer cells activating the glioma-associated transcription factors (Gli) in surroundin
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qx 314 Analysis of the GHSR screening data for inactive
2022-03-14
Analysis of the GHSR screening data for inactive library members indicated that the prolinol-derived secondary amine and α-substituted phenoxyacetamide moieties described in were critical for activity. As a result, we initiated the synthesis of follow-up libraries utilizing the solid-phase chemistry
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Type II diabetes is characterized by an
2022-03-14
Type II diabetes is characterized by an inability to maintain glucose homeostasis due to insulin desensitization and/or insufficient insulin secretion. GPR40, also known as free fatty kinesin spindle protein receptor 1 (FFAR1), is a member of the G-protein-coupled lipid-activated family of receptor
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To evaluate the role of increased FPPS
2022-03-14
To evaluate the role of increased FPPS expression in paclitaxel-treated cells, we investigated the effects of FPPS on chemokine receptor antagonist progression. DNA content analysis showed that the number of cells accumulating in the G/M phase increased in a dose-dependent manner in paclitaxel-trea
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We also intended to determine the possible mechanism underly
2022-03-14
We also intended to determine the possible mechanism underlying EZH2 upregulation in the PC. Although no recurrent mutations of EZH2 have been described in CLL [27, 28, 29], we aimed to rule out the possibility of activating mutations in the background of EZH2 overexpression. We detected no mutation
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With the increasing use of
2022-03-14
With the increasing use of INSTIs in clinical practice, drug resistance to this class in different HIV-1 subtypes should be carefully monitored and investigated. Studies on HIV-1 diversity and drug resistance would greatly help our understanding of viral transmission, pathogenesis and ART resistance
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Although HK localizes mainly to either the cytosol or mitoch
2022-03-14
Although HK localizes mainly to either the cytosol or mitochondria [29], [30], [31] and cardioprotection is associated with increased mitochondrial HK binding, some studies have identified a component of HK located in intracellular vesicles within the cardiomyocyte [48], [61], supporting older data
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Based on the in vitro findings summarized here we posited
2022-03-14
Based on the in vitro findings summarized here, we posited that, in the intact brain, release of ROS from iron-laden astrocytes to the local neuropil elicits oxidative damage and degeneration of indigent dopaminergic projections and other vulnerable neuronal elements (Schipper, 2001). Of particular
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Previous studies have established that phosphorylation of GC
2022-03-14
Previous studies have established that phosphorylation of GC-B is required for activation of GC-B. Conversion of all six chemically determined serine and threonine phosphorylation sites in GC-B to alanines produced a properly folded enzyme that retained GC activity under synthetic detergent activati
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br Biochemical properties and post translational modificatio
2022-03-14
Biochemical properties and post-translational modification of GCAPs GCAPs are hydrophobic proteins that are likely permanently bound to their GC target under physiological conditions [5]. They interact with the photoreceptor GCs through the intracellular domains (reviewed in [17]). GCAP1 has been
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br Conclusions br Introduction Astrocytes
2022-03-14
Conclusions Introduction Astrocytes contribute to physiological AICAR phosphate function on many levels. They help maintain the physiological composition of the extracellular medium by, for instance, buffering potassium and uptake of neurotransmitters. They can also provide neurons with energ
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