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To test our refinement protocol we considered
2022-01-06

To test our refinement protocol, we considered a benchmark set of 12 N-linked glycan-containing protein structures determined by X-ray crystallography at resolutions ranging between 1.9 Å and 3.5 Å and comprising a total of 133 glycan units. We identified four incorrect anomeric configurations and 2
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Herein in consider of the high similarity between GR
2022-01-06

Herein, in consider of the high similarity between GR HBP site and AR HBP site, we applied rational drug design strategy to develop AR/GR antagonists based on the chemical structures of antiandrogens and crystal structure of GR. The following bioassay identified Z19 as a dual AR/GR antagonist. Z19 i
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The expression and localization of Cx Cx and Cx
2022-01-06

The expression and localization of Cx43, Cx46 and Cx50 in the anterior pituitary vary with physiological activities and with various conditions associated with both natural and pathological changes in hormone secretion. Anterior pituitary Cx43 and Cx50 levels increase and exhibit a more widespread d
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Recently there are only a spot
2022-01-06

Recently, there are only a spot of FFA4 agonists reported in the literature (Fig. 1),13, 14, 15 and there is no selective FFA4 agonists have reached clinical trial for the treatment of T2DM. TUG-891, the first potent and selective FFA4 agonist, was developed in University of Southern Denmark as a wi
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br Short Communication Free fatty acid receptors
2022-01-06

Short Communication Free fatty BHQ receptors (FFAR) play significant roles in energy metabolism (Brown et al., 2005; Ichimura et al., 2009). The receptor FFAR1 is involved in insulin secretion in humans (Meidute Abaraviciene et al., 2013). Activation of the receptor FFAR2 increases lipid accretio
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br Materials and methods br Results and discussion br Conclu
2022-01-06

Materials and methods Results and discussion Conclusions Acknowledgments The authors are grateful to Dr. N. Prevete for providing the human AGS shCTR and AGS shFPR2 cells. This work was supported by POR Campania FSE 2007-2013 Project CREME and Ministry of Health, Italy, RF-2011-02349269.
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FPR activation stimulates multiple signal transduction pathw
2022-01-06

FPR1 activation stimulates multiple signal transduction pathways responsible for various neutrophil functions, such as adhesion, chemotaxis, phagocytosis, leukotriene receptor agonist of secretory granules, and superoxide anion radical (O2) production, which contribute to the physiological inflammat
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Although our knowledge of how FAs
2022-01-06

Although our knowledge of how FAs affect GLP-1-producing L-cells is sparse and incomplete, increased intracellular ceramide [6], ER stress [12], and increased production of ROS [9] are indicated mediators of the lipotoxicity induced by SFA (16:0). However, the role for/interaction between these medi
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In cardiomyocytes mechanical stress builds up
2022-01-06

In cardiomyocytes mechanical stress builds up via FAs and the related costamere structures, and excessive stress can cause cardiac hypertrophy. Cardoso et al. (2016) report a comprehensive study that demonstrates the link between stress-induced FAK activation and a FAK-mediated initiation of a trans
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Factor Xa FXa has emerged as
2022-01-06

Factor Xa (FXa) has emerged as a particularly promising target for the development of effective anticoagulant drugs because FXa acts at the convergence point of the extrinsic and intrinsic coagulation pathways. It efficiently catalyzes the conversion of prothrombin to thrombin with one molecule of F
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Aberrant activity of PRC as a result of
2022-01-06

Aberrant activity of PRC2 as a result of over expressed EZH2, has been frequently seen in a wide range of human cancers including breast and prostate tumors [10]. However, leukemia-associated epigenetic aberrations are not fully understood [7]. Herein, we will overview the current knowledge of epige
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Previous studies have shown that
2022-01-06

Previous studies have shown that inhibition of voltage-gated Na+ Insulin (human) recombinant expressed in yeast has a reduced effect on GABAergic boutons compared with other neurotransmitter phenotypes,46, 47 and voltage-gated Na+ channel subtypes are differentially expressed in hippocampus. In addi
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FG4592 br Cellular transportation of nanoparticles and nanoc
2022-01-06

Cellular transportation of nanoparticles and nanocomplexes Endocytosis and exocytosis are critically important phenomena in cellular metabolism, which involve the complex vesicular system. They deal with major cellular transportation activities including membrane homeostasis by transporting prote
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LSD also contributes to the regulation of specific programs
2022-01-06

LSD1 also contributes to the regulation of specific programs of gene expression in postmitotic, fate-committed neurons. Perhaps its most specialized role is in the complex series of epigenetic regulatory events that permit each olfactory sensory neuron to express one and only one of the thousands of
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SAR around amino derivative revealed a number of
2022-01-05

SAR around amino-derivative revealed a number of interesting trends related to the serum shift and in vitro activity (). A comparison of derivative , and its epimer , showed that the stereochemistry had little effect on the serum shift and the intrinsic affinity for the receptor. In contrast, re-p
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