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In an attempt to further optimize interactions in
2021-11-01
In an attempt to further optimize interactions in the lipophilic P4 pocket, we next prepared compounds – () which possessed the preferred stereochemistry at P4, but with R-groups of varying size and shape. In addition to providing important structural information for maximizing potency, these compou
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The initial beta carboline derivatives used in the
2021-11-01
The initial beta-carboline derivatives used in the in silico docking experiments were prepared using the procedure outlined in . Harmol, , was -alkylated with -Boc-protected alkylamines in the presence of cesium carbonate to give and . The carbamate protecting group was removed under acidic conditi
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apigenin mg Interestingly in vivo infusion and uptake of Ang
2021-11-01
Interestingly, in vivo infusion and uptake of Ang II in intact mice indicated that multiligand endocytic receptor megalin has at least some role in the uptake of Ang II and the downstream signaling process in proximal tubule apigenin mg (PTCs) in vivo [173]. Earlier in vivo studies showed that PTCs
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Cepharanthine synthesis Dormancy is a physiological state wh
2021-11-01
Dormancy is a physiological state when viable seeds do not germinate. Seed stratification, a commonly used technique, is used for dormancy removal and can be performed in moisture for an experimentally revealed time at warm or cold temperatures. All conditions depends on plant species (Dębska et al.
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A main finding of this study was that the impact
2021-11-01
A main finding of this study was that the impact of exogenous insulin on hippocampal memory and glucose utilization was GluT4-dependent. Although insulin was administered directly to the hippocampus, it is important to point out that such administration does indeed have physiological relevance; that
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br Genetic manipulation variation of the ghrelin system
2021-11-01
Genetic manipulation/variation of the ghrelin system and alcohol-related outcomes Genetic manipulation of the ghrelin system (either the peptide or the receptor gene) via knockout rodent models has provided further insight into the role of this system in alcohol seeking and consummatory behaviors
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br Materials and methods br Results Bgal from Alteromonas sp
2021-11-01
Materials and methods Results Bgal from Alteromonas sp. ML117 had an open reading frame of 3126 bp encoding 1042 amino wee1 residues with a predicted mass of 120 kDa and a theoretical pI (isoelectric point) of 5.44. The recombinant Bgal contained a His tag, as well as other additional amino a
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Glucose metabolic pathways are well defined but
2021-11-01
Glucose metabolic pathways are well defined but the subcellular organization of these pathways is poorly understood in liver and kidney. Several factors affect the net flux of gluconeogenesis and allow the opioid receptor to respond to physiological changes [1]. Ovadi and Srere have suggested that
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Despite these data implicating Kdm b as
2021-11-01
Despite these data implicating Kdm6b as a positive regulator of neuronal differentiation, and surprisingly, given the evidence that germline knockouts die perinatally due to an inability to breathe, the brains of Kdm6b knockout mice are remarkably normal in gross morphology [26,]. Interestingly, Kdm
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We also conducted analyses on the
2021-11-01
We also conducted analyses on the functional category of UP_Keywords and on KEGG pathways for further understanding. The UP_Keywords analysis (D) demonstrated that acetylation and phosphoprotein were highly enriched categories. KEGG pathways categories (E) of ribosome biogenesis in eukaryotes, DNA r
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In diseased blood vessels increased production of reactive o
2021-10-29
In diseased blood vessels, increased production of reactive oxygen species (ROS), such as peroxynitrite, superoxide, and hydrogen peroxide, have been found [[53], [54], [55]]. Peroxynitrite was suggested to alter the redox state of sGC [53] while hydrogen peroxide interfered with the action of NO bu
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1423 receptor As part of their ongoing effort
2021-10-29
As part of their ongoing effort in the field, Kalypsis recently disclosed that quinazolinones 5 [49], imidazo[1,2-a] [1,2]diazepin 6 [50] and quinolines 7 [51] all had activity as small molecule modulators of TGR5 (Figure 4). Intercept, however, disclosed different bile 1423 receptor derivatives as
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Glycogen synthase kinase GSK is
2021-10-29
Glycogen synthase kinase 3 (GSK3) is currently considered to be a multifunctional serine/threonine kinase involved in a wide spectrum of cellular processes such as glycogen metabolism, cell proliferation, neuronal function, oncogenesis or embryonic development (for recent reviews see: Rayasam et al.
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In summary activated A AR exacerbated the reverse
2021-10-29
In summary, activated A2AR exacerbated the reverse transport function of endothelial EAATs through a direct or indirect pathway depending on PKA and glutamate levels in response to OGD in vitro, but A2AR inhibition quickly restored the normal transport function. Moreover, the key mechanisms by which
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We report on four affected children from two unrelated
2021-10-29
We report on four affected children from two unrelated consanguineous hydroxylase inhibitor with moderate to severe ID associated with epilepsy and variable neuropsychiatric features. Using whole-exome sequencing, we identified homozygous missense variants in SLC45A1 (OMIM: 605763), which codes for
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